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United States Patent 5,152,824
Makino ,   et al. October 6, 1992

Sulfamidosulfonamide derivatives and herbicides

Abstract

A sulfamidosulfonamide derivative of the formula (1) and an agriculturally suitable salt thereof: ##STR1## wherein Q is ##STR2## X is an oxygen atom or a sulfur atom; and G is ##STR3## which are useful as herbicide.


Inventors: Makino; Kenzi (Funabashi, JP); Morimoto; Katsushi (Funabashi, JP); Akiyama; Shigeaki (Funabashi, JP); Suzuki; Hideaki (Funabashi, JP); Nagaoka; Takeshi (Funabashi, JP); Suzuki; Koichi (Shiraoka, JP); Nawamaki; Tsutomu (Shiraoka, JP); Watanabe; Shigeomi (Shiraoka, JP)
Assignee: Nissan Chemical Industries Ltd. (Tokyo, JP)
Appl. No.: 665557
Filed: March 6, 1991
Foreign Application Priority Data

Mar 06, 1990[JP]2-54455
Mar 06, 1990[JP]2-54456
Jun 12, 1990[JP]2-153345
Nov 06, 1990[JP]2-300127
Dec 19, 1990[JP]2-403735

Current U.S. Class: 504/222; 504/219; 504/223; 504/235; 504/239; 504/240; 504/247; 504/253; 504/264; 504/265; 504/266; 504/267; 504/269; 504/270; 504/271; 504/276; 504/280; 504/282; 544/8; 544/60; 544/140; 546/211; 546/268.7; 546/272.1; 546/275.4; 548/127; 548/365.4; 548/365.7; 548/374.1; 548/376.1; 548/379.1; 548/379.4
Intern'l Class: A01N 043/02; A01N 043/48; A01N 043/64; C07D 285/16
Field of Search: 544/8,60,140 548/375,378,127 546/211,279 71/92,91


References Cited
U.S. Patent Documents
4629495Dec., 1986Hatton et al.71/92.
Foreign Patent Documents
37482Oct., 1981EP.

Primary Examiner: Shah; Mukund J.
Assistant Examiner: Grumbling; Matthew V.
Attorney, Agent or Firm: Oblon, Spivak, McClelland, Maier & Neustadt

Claims



We claim:

1. A sulfamidosulfonamide derivative of the formula (1) and an agriculturally suitable salt thereof: ##STR172## Wherein Q is ##STR173## whereinR.sup.11 is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.3-7 cycloalkyl group, a C.sub.1-6 alkyl group substituted by a C.sub.3-7 cycloalkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 mono- or poly-halogenoalkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylthio group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylsulfonyl group, a C.sub.1-6 mono- or polyhalogenoalkyl group, a C.sub.1-6 alkyl group substituted by a cyano group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylcarbonyl group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C.sub.1-6 alkyl group, a C.sub. 1-6 alkoxy group and a C.sub.1-6 alkoxycarbonyl group);

R.sup.12 is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group and a C.sub.1-6 alkoxycarbonyl group);

R.sup.13 is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a C.sub.1-6 alkoxycarbonyl group and a nitro group); or, R.sup.12 and R.sup.13 form, together with the nitrogen atom to which they are bonded, a saturated 5-7-membered heterocyclic group;

or, R.sup.12 and R.sup.13 form, together With the oxygen atom and the nitrogen atom to which they are bonded, a saturated 5-7-membered heterocyclic group;

R.sup.21 ; is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 mono- or poly-halogenoalkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylthio group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylsulfonyl group, a C.sub.1-6 mono- or poly-halogenoalkyl group, a C.sub.1-6 alkyl group Substituted by a cyano group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylcarbonyl group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a C.sub.1-6 alkoxycarbonyl group and a nitro group);

R.sup.22 is a hydrogen atom or a C.sub.1-6 alkyl group;

R.sup.23 is a hydrogen atom or a C.sub.1-6 alkyl group;

R.sup.24 is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a halogen atom, a C.sub.1-6 mono- or poly-halogenoalkyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.2-6 alkenyloxy group, a C.sub.1-6 alkyl group substituted by a C.sub.2-6 alkynyloxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 mono- or poly-halogenoalkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylthio group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylsulfonyl group, a C.sub.1-6 alkyl group substituted by a cyano group, a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkylcarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylcarbonyl group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a C.sub.1-6 alkoxycarbonyl group and a nitro group);

R.sup.25 is a hydrogen atom or a C.sub.1-6 alkyl group;

R.sup.26 is a hydrogen atom or a C.sub.1-6 alkyl group;

R.sup.27 is a hydrogen atom or a C.sub.1-6 alkyl group;

R.sup.28 is a hydrogen atom, a halogen atom, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.1-6 mono- or poly-halogenoalkyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.2-6 alkenyloxy group, a C.sub.1-6 alkyl group substituted by a C.sub.2-6 alkynyloxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylthio group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylsulfonyl group, a C.sub.1-6 alkyl group substituted by a cyano group, a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkylcarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylcarbonyl group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a C.sub.1-6 alkoxycarbonyl group and a nitro group);

X is an oxygen atom or a sulfur atom;

G is ##STR174## wherein each of a, b, c and d, which are independent from one another, is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.1-6 alkyl group mono- or poly-substituted by a halogen atom, a C.sub.1-6 alkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxy group, a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylthio group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylsulfonyl group, a C.sub.1-6 alkylthio group, a C.sub.1-6 alkylcarbonyl group, a C.sub.3-7 cycloalkyl group, a C.sub.3-7 cycloalkenyl group, a cyano group, a nitro group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a C.sub.1-6 alkoxycarbonyl group and a nitro group), a 5- or 6-membered heterocyclic group (provided that such a heterocyclic group contains from 1 to 3 hetero atoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atoms in the ring, or contains a sulfonyl group, and such a heterocyclic group may be substituted by one or more substituents selected from the group consisting of a C.sub.1-6 alkyl group, a C.sub. 1-6 alkoxy group, a halogen atom, a trifluoromethyl group, a nitro group and a C.sub.1-6 alkoxycarbonyl group), a naphthyl group, a benzene-condensed heterocyclic group (provided that such a benzene-condensed heterocyclic group contains 1 or 2 hetero atoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atoms, and such a benzene-condensed heterocyclic group may be substituted by one or more substituents selected from the group consisting of a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a halogen atom, a trifluoromethyl group, a nitro group and a C.sub.1-6 alkoxycarbonyl group).

2. A selective herbicide containing one or more compounds defined in claim 1 as active ingredients.

3. A herbicidal composition comprising a herbicidally effective amount of one or more compounds defined in claim 1 and an agricultural adjuvant.

4. A herbicidal composition comprising a herbicidally effective amount of one or more compounds of formula I ##STR175## wherein Y is a member selected from the group consisting of phenyl, substituted phenyl which may be substituted with F, Cl, or OCH.sub.3, and thienyl,

Z is hydrogen or methyl,

Q' is ##STR176## and an agricultural adjuvant

5. A herbicidal composition comprising a herbicidally effective amount of one or more compounds of formula I as defined in claim 4, wherein Q' is ##STR177## and an agricultural adjuvant.

6. A herbicidal composition comprising a herbicidally effective amount of one or more compounds of formula I as defined in claim 4, wherein Q' is ##STR178## and an agricultural adjuvant.

7. A herbicidal composition comprising a herbicidally effective amount of a compound of formula I as defined in claim 5, wherein Y is phenyl, Z is methyl, and an agricultural adjuvant.
Description



TECHNICAL FIELD

The present invention relates to novel sulfamidosulfonamide derivatives and agriculturally suitable salts thereof, and herbicides containing them as active ingredients.

BACKGROUND TECHNIQUE

It is indispensable to use herbicides to protect important crop plants such as rice, wheat, corn, soybean, cotton and sugar beet from weeds and thereby to increase the harvest. Especially in recent years, a selective herbicide is desired which is capable of selectively killing weeds without showing any phytotoxicity against crop plants when applied to the foliages of crop plants and weeds simultaneously in a field where such useful crop plants and weeds are coexistent. Further, with a view to avoiding environmental pollution and reducing the costs for transportation and application, researches and developments have been conducted for many years for compounds having high herbicidal effects at low doses. Some of the compounds having such properties are presently used as selective herbicides. However, there still exists a need for better compounds having such properties.

As the prior art showing a chemical structure similar to that of the compounds of the present invention, Japanese Unexamined Patent Publication No. 45473/1990 discloses substituted sulfonyldiamides, and Japanese Unexamined Patent Publication No. 122671/1988 discloses 1-carbamoyl-2-pyrazolines. However, sulfamidosulfonamide derivatives having a pyrazoline structure like the compounds of the present invention have not been known at all, and they are novel compounds.

DISCLOSURE OF THE INVENTION

The present inventors have conducted extensive researches over years to develop selective herbicides for important crop plants and have studied herbicidal properties of many compounds with an aim to find out compounds having higher herbicidal activities as well as selectivity. As a result, it has been found that sulfamidosulfonamide derivatives of the following formula (1) and agriculturally suitable salts thereof (hereinafter referred to as the compounds of the present invention) exhibit remarkably strong herbicidal activities against many weeds in soil treatment or in foliage treatment and at the same time have a high level of safety for important crop plants such as wheat, corn, cotton, soybean, sugar beet and rice. The present invention has been accomplished on the basis of this discovery. On the other hand, since the compounds of the present invention show high herbicidal activities at a very low dose as compared with conventional herbicides, they are also useful as herbicides for orchards or for non-agricultural fields.

Namely, the present invention provides a sulfamidosulfonamide derivative of the formula (1) and an agriculturally suitable salt thereof: ##STR4## wherein Q is ##STR5## wherein R.sup.11 is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.3-7 cycloalkyl group, a C.sub.1-6 alkyl group substituted by a C.sub.3-7 cycloalkyl group, a C.sub.2-6 alkenyl group, a C.sub.1-6 alkynyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 mono- or poly-halogenoalkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylthio group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylsulfonyl group, a C.sub.1-6 mono- or poly-halogenoalkyl group, a C.sub.1-6 alkyl group substituted by a cyano group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylcarbonyl group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group and a C.sub.1-6 alkoxycarbonyl group);

R.sup.12 is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group and a C.sub.1-6 alkoxycarbonyl group);

R.sup.13 is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.1-6 alkynyl group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a C.sub.1-6 alkoxycarbonyl group and a nitro group);

or, R.sup.12 and R.sup.13 form, together with the nitrogen atom to which they are bonded, a saturated 5-7 membered heterocyclic group;

or, R.sup.12 and R.sup.13 form, together with the oxygen atom and the nitrogen atom to which they are bonded, a saturated 5-7 membered heterocyclic group;

R.sup.21 is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 mono- or poly-halogenoalkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylthio group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylsulfonyl group, a C.sub.1-6 mono- or poly-halogenoalkyl group, a C.sub.1-6 alkyl group substituted by a cyano group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylcarbonyl group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a C.sub.1-6 alkoxycarbonyl group and a nitro group);

R.sup.22 is a hydrogen atom or a C.sub.1-6 alkyl group;

R.sup.23 is a hydrogen atom or a C.sub.1-6 alkyl group;

R.sup.24 is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a halogen atom, a C.sub.1-6 mono- or poly-halogenoalkyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.2-6 alkenyloxy group, a C.sub.1-6 alkyl group substituted by a C.sub.2-6 alkynyloxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 mono- or poly-halogenoalkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylthio group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylsulfonyl group, a C.sub.1-6 alkyl group substituted by a cyano group, a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkylcarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylcarbonyl group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a C.sub.1-6 alkoxycarbonyl group and a nitro group);

R.sup.25 is a hydrogen atom or a C.sub.1-6 alkyl group;

R.sup.26 is a hydrogen atom or a C.sub.1-6 alkyl group;

R.sup.27 is a hydrogen atom or a C.sub.1-6 alkyl group;

R.sup.28 is a hydrogen atom, a halogen atom, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.1-6 mono- or poly-halogenoalkyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.2-6 alkenyloxy group, a C.sub.1-6 alkyl group substituted by a C.sub.2-6 alkynyloxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylthio group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylsulfonyl group, a C.sub.1-6 alkyl group substituted by a cyano group, a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkylcarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylcarbonyl group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a C.sub.1-6 alkoxycarbonyl group and a nitro group);

X is an oxygen atom or a sulfur atom;

G is ##STR6## wherein each of a, b, c and d, which are independent from one another, is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.1-6 alkyl group mono- or poly-substituted by a halogen atom, a C.sub.1-6 alkoxy group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkoxy group, a C.sub.1-6 alkoxycarbonyl group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylthio group, a C.sub.1-6 alkyl group substituted by a C.sub.1-6 alkylsulfonyl group, a C.sub.1-6 alkylthio group, a C.sub.1-6 alkylcarbonyl group, a C.sub.3-7 cycloalkyl group, a C.sub.3-7 cycloalkenyl group, a cyano group, a nitro group, a phenyl group or a benzyl group (provided that such a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a C.sub.1-6 alkoxycarbonyl group and a nitro group , a 5- or 6-membered heterocyclic group (provided that such a heterocyclic group contains from 1 to 3 hetero atoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atoms in the ring, or contains a sulfonyl group, and such a heterocyclic group may be substituted by one or more substituents selected from the group consisting of a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a halogen atom, a trifluoromethyl group, a nitro group and a C.sub.1-6 alkoxycarbonyl group), a naphthyl group, a benzene-condensed heterocyclic group (provided that such a benzene-condensed heterocyclic group contains 1 or 2 hetero atoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atoms, and such a benzene-condensed heterocyclic group may be substituted by one or more substituents selected from the group consisting of a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a halogen atom, a trifluoromethyl group, a nitro group and a C.sub.1-6 alkoxycarbonyl group).

The present invention also provides a selective herbicide containing one or more compounds of the present invention as active ingredients.

Further, the present invention provides a herbicidal composition comprising a herbicidally effective amount of one or more compounds of the present invention and an agricultural adjuvant.

Now, the present invention will be described in detail with reference to the preferred embodiments.

The compounds of the formula (1) of the present invention can easily be prepared by any one of the following reaction schemes 1 to 5. ##STR7## In the above formulas, Q, G and X are as defined above.

Namely, the reaction of a sulfamidosulfonyliso(thio)cyanate derivative (2) with a pyrazoline derivative (3), is conducted by using the sulfamidosulfonyliso(thio)cyanate derivative (2) in an amount of from 0.5 to 3.0 mols per mol of the pyrazoline derivative (3). Preferably the amount is within a range of from 0.8 to 1.2 mols.

The reaction temperature can be selected optionally within a range of from -50.degree. C. to 200.degree. C. However, the temperature is preferably within a range of from -20.degree. C. to 50.degree. C.

This reaction usually proceeds readily to present the compound (1) of the present invention. If the reaction tends to hardly proceed, a suitable base, for example, an organic base such as triethylamine, triethylenediamine, pyridine or 1,8-diazabicyclo[5.4.0]-7-undecene (DBU), a metal alkoxide such as sodium methoxide or sodium ethoxide, a metal hydride such as sodium hydride, an alkyl metal such as n-butyl lithium, or an inorganic base such as potassium carbonate, potassium hydroxide or sodium hydroxide, may be added to facilitate the reaction. As the base, it is particularly preferred to employ an organic base or an inorganic base.

As a solvent suitable for this reaction, a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform, carbon tetrachloride, an ether such as diethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzin or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethylphosphoric acid triamide, may be mentioned. These solvents may be used alone or in combination as a mixture.

After completion of the reaction, usual posttreatment is conducted to obtain the compound (1) of the present invention. The structure of the compound of the present invention was determined by e.g. IR, NMR or MASS. ##STR8## In the above formulas, Q, G and X are as defined above, and Y is a C.sub.1-6 alkyl group, a phenyl group or a benzyl group (provided that such an alkyl group, a phenyl group or a benzyl group may be substituted by one or more substituents selected from the group consisting of a C.sub.1-6 alkyl group, C.sub.1-6 alkoxy group and a halogen atom).

Namely, the reaction of a sulfamidosulfonamide derivative (4) with chloro(thio)formic acid ester or thio)carbonic acid diester is conducted by using the chloro(thio)formic acid ester or the (thio)carbonic acid diester in an amount of from 0.5 to 3.0 mols per mol of the sulfamidosulfonamide derivative (4). The amount is preferably within a range of from 0.8 to 1.2 mols.

The reaction temperature can be selected optionally within a range of from -50.degree. C. to 200.degree. C. However, it is preferably within a range of from -20.degree. C. to 100.degree. C.

This reaction is conducted by using various bases. The base is used in an amount of from 0.5 to 5.0 mols per mol of the sulfamidosulfonamide derivative (4). As a suitable base, an organic base such as triethylamine, triethylenediamine, pyridine, 1,8-diazabicyclo[5.4.0]-7-undecene (DBU), a metal alkoxide such as sodium methoxide or sodium ethoxide, a metal hydride such as sodium hydride, an alkyl metal such as n-butyl lithium, or an inorganic base such as potassium carbonate, potassium hydroxide or sodium hydroxide, may, for example, be used. It is particularly preferred to employ an organic base or an inorganic base.

As a solvent suitable for this reaction, a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as diethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzin or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethylphosphoric acid triamide, may be mentioned. These solvents may be used alone or in combination as a mixture.

After completion of the reaction, usual posttreatment is conducted to obtain an N-sulfamidosulfonyl(thio)carbamate derivative (5).

Then, the reaction of the N-sulfamidosulfonyl(thio)carbamate derivative (5) with a pyrazoline derivative (3) is conducted by using the pyrazoline derivative (3) in an amount of from 0.5 to 10.0 mols per mol of the N-sulfamidosulfonyl(thio)carbamate derivative (5). The amount is preferably within a range of from 0.5 to 3.0 mols.

The reaction temperature can be selected optionally within a range of from 0.degree. C. to 250.degree. C. However, it is preferably within a range of from 50.degree. C. to 150.degree. C.

This reaction usually proceeds readily to present the compound (1) of the present invention. However, if the reaction tends to hardly proceed, a suitable base, for example, an organic base such as triethylamine, triethylenediamine, pyridine or 1,8-diazabicyclo[5.4.0]-7-undecene (DBU), a metal alkoxide such as sodium methoxide or sodium ethoxide, a metal hydride such as sodium hydride, an alkyl metal such as n-butyl lithium, or an inorganic base such as potassium carbonate, potassium hydroxide or sodium hydroxide, may be added to facilitate the reaction. As the base, it is particularly preferred to employ an organic base or an inorganic base.

As a solvent suitable for this reaction, a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as diethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzin or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethylphosphoric acid triamide, may be mentioned. These solvents may be used alone or in combination as a mixture.

After completion of the reaction, usual posttreatment is conducted to obtain the compound (1) of the present invention. The structure of the compound of the present invention was determined by e.g. IR, NMR or MASS. ##STR9## In the above formulas, Q, G and Y are as defined above.

Namely, the reaction of a sulfamide (7) with an N-chlorosulfonylcarbamate derivative (6) is conducted by using the N-chlorosulfonylcarbamate derivative (6) in an amount of from 0.5 to 3.0 mols per mol of the sulfamide (7) The amount is preferably within a range of from 0.9 to 1.2 mols.

The reaction temperature may be selected optionally within a range of from -50.degree. C. to 100.degree. C. However, it is preferably within a range of from -20.degree. C. to 30.degree. C.

This reaction can be conducted by using various bases. The base is used in an amount of from 0.5 to 4.0 mols per mol of the sulfamide (7). As a suitable base, a metal hydride such as sodium hydride, a metal alkoxide such as sodium methoxide or sodium ethoxide, an alkyl metal such as n-butyl lithium, an organic base such as triethylamine, triethylenediamine, pyridine or 1,8-diazabicyclo[5.4.0]-7-undecene (DBU), or an inorganic base such as potassium carbonate, potassium hydroxide or sodium hydroxide, may be employed. It is particularly preferred to employ a metal hydride, an organic base or an inorganic base.

As a solvent suitable for this reaction, a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as diethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzin or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethylphosphoric acid triamide, may be mentioned. These solvents may be used alone or in combination as a mixture. It is particularly preferred to employ an ether or an amide.

After completion of the reaction, usual posttreatment is conducted to obtain an N-sulfamidosulfonylcarbamate derivative (5; X=0).

Then, the reaction of the N-sulfamidosulfonylcarbamate derivative (5; X=0) with a pyrazoline derivative (3) is conducted by using the pyrazoline derivative (3) in an amount of from 0.5 to 10.0 mols per mol of the N-sulfamidosulfonylcarbamate derivative (5; X=0). The amount is preferably within a range of from 0.5 to 3.0 mols.

The reaction temperature can be selected optionally within a range of from 0.degree. C. to 250.degree. C. However, it is preferably within a range of from 50.degree. C. to 150.degree. C.

This reaction usually proceeds readily to present the compound (1) of the present invention. However, if the reaction tends to hardly proceed, a suitable base, for example, an organic base such as triethylamine, triethylenediamine, pyridine or 1,8-diazabicyclo[5.4.0]-7-undecene (DBU), a metal alkoxide such as sodium methoxide or sodium ethoxide, metal hydride such as sodium hydride, an alkyl metal such as n-butyl lithium, or an inorganic base such as potassium carbonate, potassium hydroxide or sodium hydroxide, may be added to facilitate the reaction. As the base, it is particularly preferred to employ an organic base or an inorganic base.

As a solvent suitable for this reaction, a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as diethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzin or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethylphosphoric acid triamide, may be mentioned. These solvents may be used alone or in combination as a mixture.

After completion of the reaction, usual posttreatment is conducted to obtain the compound (1; X=0) of the present invention. The structure of the compound of the present invention was determined by e.g. IR, NMR or MASS. ##STR10## In the above formulas, Q, G and Y are as defined above.

Namely, the reaction of a sulfamidosulfonamide derivative (4) with a pyrazolinylformic acid ester (8) is conducted by using the pyrazolinylformic acid ester (8) in an amount of from 0.5 to 3.0 mols per mol of the sulfamidosulfonamide derivative (4). The amount is preferably within a range of from 0.8 to 1.2 mols.

The reaction temperature can be selected optionally within a range of from -50.degree. C. to 100.degree. C.

This reaction can be conducted by using various bases. The base is used in an amount of from 0.5 to 4.0 mols per mol of the sulfamidosulfonamide derivative (4). As a suitable base, an organic base such as triethylamine, triethylenediamine, pyridine or 1,8-diazabicyclo[5.4.0]-7-undecene (DBU), an inorganic base such as potassium carbonate, potassium hydroxide or sodium hydroxide, an alkyl metal such as n-butyl lithium or trimethyl aluminum, a metal hydride such as sodium hydride, or a metal alkoxide such as sodium methoxide or sodium ethoxide, may be employed. It is particularly preferred to employ an organic base, an inorganic base or an alkyl metal.

As a solvent suitable for this reaction, a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as diethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzin or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethylphosphoric acid triamide, may be mentioned. These solvents may be used alone or in combination as a mixture.

After completion of the reaction, usual posttreatment is conducted to obtain the compound (1; X=0) of the present invention. The structure of the compound of the present invention was determined by e.g. IR, NMR or MASS. ##STR11## In the above formulas, Q and G are as defined above.

Namely, the reaction of a pyrazoline derivative (3) with a chlorosulfonyl isocyanate is conducted by using the chlorosulfonyl isocyanate in an amount of from 0.5 to 3.0 mols per mol of the pyrazoline derivative (3). The amount is preferably within a range of from 0.8 to 1.2 mols.

The reaction temperature can be selected optionally within a range of from -50.degree. C. to 100.degree. C. However, it is preferably within a range of from -30.degree. C. to 50.degree. C.

As a solvent suitable for this reaction, a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as diethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzin or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethylphosphoric acid triamide, may be mentioned. These solvents may be used alone or in combination as a mixture.

This reaction usually proceeds readily without using a base.

Then, a suitable base is added to the reaction system of the pyrazoline derivative (3) and the chlorosulfonyl isocyanate, and a sulfamide derivative (7) is reacted to obtain a compound of the present invention (1; X=0). The base is used in an amount of from 0.5 to 4.0 mols, preferably from 0.8 to 2.2 mols, per mol of the pyrazoline derivative (3). Further, the sulfamide derivative (7) is used in an amount of from 0.5 to 2.0 mols, preferably from 0.8 to 1.2 mols, per mol of the pyrazoline derivative (3).

As a suitable base, an organic base such as triethylamine, triethylenediamine, pyridine or 1,8-diazabicyclo[5.4.0]-7-undecene (DBU), an inorganic base such as potassium carbonate, potassium hydroxide or sodium hydroxide, an alkyl metal such as n-butyl lithium, a metal hydride such as sodium hydride, or a metal alkoxide such as sodium methoxide or sodium ethoxide, may be employed. It is particularly preferred to employ an organic base, an inorganic base or a metal hydride.

The reaction temperature can be selected optionally within a range of from -50.degree. C. to 150.degree. C. However, it is preferably within a range of from -30.degree. C. to 60.degree. C.

After completion of the reaction, usual posttreatment is conducted to obtain the compound (1; X=0) of the present invention. The structure of the compound of the present invention was determined by e.g. IR, NMR or MASS.

The sulfamidosulfonyliso(thio)cyanate derivative (2) to be used in the Reaction scheme 1, can be prepared from the sulfamide derivative (7) or the sulfamidosulfonamide derivative (4) in accordance with the method disclosed in e.g. Japanese Unexamined Patent Publications No. 45473/1990, No. 151577/1989, No. 31775/1984, No. 148879/1983, No. 13266/1980 and No. 81320/1974.

Further, the sulfamidosulfonamide derivative (4) can be prepared from the sulfamide derivative (7) in accordance with the following Reaction schemes 6 and 7. ##STR12## In the above formulas, Q is as defined above.

In the Reaction scheme 6, removal of the tert-butyl group is conducted by using trifluoroacetic acid.

The amount of trifluoroacetic acid can be selected optionally from an equimolar amount to excess amount. Further, trifluoroacetic acid may be used as a solvent without any problem.

The reaction temperature can be selected optionally within a range of from -50.degree. C. to 80.degree. C. It is preferably within a range of from -20.degree. C. to 30.degree. C.

In a case where a solvent is employed in this reaction, a solvent inert to the reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as diethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzin or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethylphosphoric acid triamide, may be used. These solvents may be used alone or in combination as a mixture. ##STR13## In the above formulas, Q is as defined above.

In the Reaction scheme 7, the reaction of t-butanol with chlorosulfonyl isocyanate can be conducted by a method per se known, such as the one disclosed in Japanese Unexamined Patent Publication No. 101323/1975.

The reaction of sulfamide (7) with tert-butyl sulfamoyl chloride is conducted by using tert-butyl sulfamoyl chloride in an amount of from 0.5 to 3.0 mols per mol of the sulfamide (7).

The reaction temperature can be selected optionally within a range of from -50.degree. C. to 100.degree. C. However, it is preferably within a range of from -20.degree. C. to 30.degree. C.

This reaction can be conducted by using various bases. The base is used in an amount of from 0.5 to 4.0 mols per mol of the sulfamide (7). The amount is preferably within a range of from 0.8 to 2.2 mols. As a suitable base, a metal hydride such as sodium hydride, a metal alkoxide such as sodium ethoxide, an alkyl metal such as n-butyl lithium, an organic base such as triethylamine, pyridine or 1,8-diazabicyclo[5.4.0]-7-undecene, or an inorganic base such as potassium hydroxide, sodium hydroxide or potassium carbonate, may be employed.

As a solvent suitable for this reaction, a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as diethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzin or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethylphosphoric acid triamide, may be mentioned. These solvents may be used alone or in combination as a mixture. It is particularly preferred to employ an ether or an amide.

In the Reaction scheme 3, the N-chlorosulfonylcarbamate derivative (6) can be prepared by a method per se known in accordance with e.g. Chemishe Berichte, vol. 96, p. 56 (1963).

The sulfamide (7) to be used as the starting material for the above reactions, can readily be prepared in accordance with e.g. Synthetic organic Chemistry, Japan, vol. 27 (No. 10), p. 980 (1969); U.S. Pat. No. 2,624,729; Chemishe Berichte, vol. 111, p. 1915 (1978); Japanese Unexamined Patent Publications No. 208289/1983, No. 79894/1978; Indian Journal of Chemistry, Section B, vol. 21B, p. 941 (1982); Journal of the American Chemical Society, vol. 66, p. 1242 (1944); U.S. Pat. No. 2,826,594.

As typical examples, syntheses of 2,4-dimethyl-1,2,5-thiadiazolidine-1,1-dioxide, 2-methoxy-1,2,5-thiadiazolidine-1,1-dioxide, N,N-dimethyl-N'-ethylsulfamide, N,N-dimethyl-N'-methoxysulfamide and N-methyl-N-methoxy-N'-ethylsulfamide, will be described by Reaction schemes 8 to 12: ##STR14##

The pyrazoline derivative (3) to be used as a starting material in the above reactions can readily be prepared in accordance with e.g. Japanese Unexamined Patent Publication No. 122671/1988; U.S. Pat. No. 3,322,831; Journal of the American Chemical Society, vol. 80, p. 1926 (1958); Chemishe Berichte, vol. 35, p. 968 (1902); Shin Jikken Kagaku Koza, vol. 14, p. 1423. Typical Examples will be described by Reaction Schemes 13 to 21: ##STR15##

Now, preparation of the compounds of the present invention will be described in further detail with reference to Reference Examples and Examples. However, it should be understood that the present invention is by no means restricted by such specific Examples.

REFERENCE EXAMPLE 1

Preparation of phenyl N-[(N-dimethylsulfamoyl-N-methyl amino)sulfonyl]carbamate ##STR16##

4.0 g (100 mmol) of 60% sodium hydride was washed with n-hexane and suspended in 100 ml of dry tetrahydrofuran (THF). Then, 6.9 g (50 mmol) of N,N,N'-trimethylsulfamide dissolved in 20 ml of dry THF was added thereto under cooling with ice, and the mixture was gradually heated and stirred at room temperature for 3 hours.

Then, 50 ml of a dry THF solution containing 13.0 g (55 mmol) of phenyl N-chlorosulfonylcarbamate was dropwise added thereto under cooling with ice, and the mixture was gradually heated to room temperature and then stirred at room temperature for 3 hours.

The reaction mixture was poured into 1000 ml of ice water containing 1.05 g of 35% hydrochloric acid and extracted with diethyl ether. The diethyl ether layer was washed sequentially with water and a saturated sodium chloride aqueous solution and then dried over anhydrous magnesium sulfate. Then, the solvent was distilled off under reduced pressure to obtain 16.0 g of phenyl N-[(N-dimethylsulfamoyl-N-methylamino)sulfonyl]carbamate as slightly yellow oil.

REFERENCE EXAMPLE 2

Preparation of phenyl N-[(N-dimethylsulfamoyl-N-methoxyamino)sulfonyl]carbamate ##STR17##

2.69 g (61.5 mmol) of 55% sodium hydride was washed with n-hexane and then suspended in 100 ml of dry THF. Then, 4.62 g (30 mmol) of N,N-dimethyl-N'-methoxysulfamide dissolved in 20 ml of THF was dropwise added thereto under cooling with ice. The mixture is heated to room temperature and then stirred at room temperature for one hour. Then, this reaction mixture was again cooled with ice, and 7.07 g (30 mmol) of phenyl N-chlorosulfonylcarbamate dissolved in 30 ml of dry THF was dropwise added thereto. The mixture was heated to room temperature and then stirred at room temperature for 30 minutes. The reaction mixture was poured into 500 ml of ice water containing 6.4 g of 35% hydrochloric acid and extracted three times with 80 ml of diethyl ether. The extract solution was washed three times with 100 ml of water and once with 100 ml of a saturated sodium chloride aqueous solution and then dried over anhydrous magnesium sulfate. Then, the solvent was distilled off under reduced pressure to obtain 10.1 g of phenyl N-[(N-dimethylsulfamoyl-N-methoxyamino)sulfonyl]carbamate as slightly yellow oil.

REFERENCE EXAMPLE 3

Preparation of phenyl N-[(N-(N-methyl-N-methoxyaminosulfonyl)-N-methylamino)sulfonyl]carbamate ##STR18##

A mixture comprising 7 g (63 mmol) of methylsulfamic acid, 13.2 g (63 mmol) of phosphorus pentachloride and 100 ml of dry benzene, was refluxed for one hour. The reaction mixture was left to cool, and the solvent was distilled off under reduced pressure to obtain 7.63 g of methylsulfamoyl chloride.

5.75 g (58.9 mmol) of N,O-dimethylhydroxylamine hydrochloride was suspended in 300 ml of dichloromethane, and 11.9 g (118 mmol) of triethylamine was added thereto. Then, the mixture was cooled with ice, and a dichloromethane solution of 7.63 g of methylsulfamoyl chloride was dropwise added, and the mixture was stirred at room temperature for 3 hours. The solvent was distilled off under reduced pressure. To the residue, 200 ml of benzene was added, and insoluble substance was filtered off. Then, the solvent was distilled off again under reduced pressure. By the distillation under reduced pressure, 4.4 g of N,N'-dimethyl-N'-methoxysulfamide was obtained (boiling point: 85.degree.-88.degree. C./1.9 mmHg).

1.15 g (28.8 mmol) of 60% sodium hydride was washed with n-hexane, and dry THF was added, and the mixture was cooled with ice. To this mixture, a THF solution containing 2 g (13 mmol) of N,N'-dimethyl-N'-methoxysulfamide was dropwise added. After stirring the mixture for 10 minutes, a dry THF solution containing 3.21 g (13.6 mmol) of phenyl N-chlorosulfonylcarbamate was dropwise added thereto. The mixture was stirred at room temperature for 7 hours. The reaction mixture was poured into 500 ml of ice water containing 3.5 g of 35% hydrochloric acid and extracted three times with diethyl ether. The diethyl ether layer was washed sequentially with water and a saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure to obtain 4.3 g of phenyl N-[(N-(N-methyl N-methoxyaminosulfonyl)-N-methylamino)sulfonyl]carbamate as slightly yellow oil.

REFERENCE EXAMPLE 4

Preparation of phenyl N-(2-methyl-tetrahydro-1,2,6-thiadiazine-1,1-dioxide-6-sulfonyl)carbamate ##STR19##

A mixture comprising 30 g (312 mmol) of sulfamide, 27.5 g (312 mmol) of N-methyl-1,3-propanediamine and 300 ml of dry pyridine was refluxed overnight at 130.degree. C. The mixture was left to cool, and then pyridine was distilled off under reduced pressure. To the residue, 200 ml of chloroform was added and insoluble substance was filtered off. The solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography (CHCl.sub.3) and then subjected to distillation under reduced pressure to obtain 36.2 g of 2-methyl-tetrahydro-1,2,6-thiadiazine-1,1-dioxide (boiling point: 130.degree.-133.degree. C./0.23 mmHg).

Then, 5.87 g (147 mmol) of 60% sodium hydride was washed twice with 30 ml of n-hexane, and then 30 ml of dry THF was added thereto, and the mixture was cooled with ice. To this mixture, a dry THF solution containing 10.0 g (66.7 mmol) of 2-methyl-tetrahydro-1,2,6-thiadiazine-1,1-dioxide was dropwise added, and the mixture was stirred at room temperature for 2.5 hours. The solution was cooled again with ice, and a dry THF solution containing 16.5 g (70 mmol) of phenyl N-chlorosulfonylcarbamate, was dropwise added thereto. The mixture was stirred at room temperature for 2 hours, and then poured into 1500 ml of ice water containing 17.4 g of 35% hydrochloric acid and extracted twice with diethyl ether. The diethyl ether layer was washed twice with water and once with a saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure to obtain 20.0 g of the desired phenyl N-(2-methyltetrahydro-1,2,6-thiadiazine-1,1-dioxide-6-sulfonyl)carbamate. Melting point: 144.degree.-145.degree. C.

The structures and physical properties or characteristics of the compounds prepared in the same manner as in the above Reference Examples 1 to 4 are shown below:

    ______________________________________
     ##STR20##                 Slightly yellow oil
     ##STR21##                 Slightly yellow oil
     ##STR22##                 Slightly yellow oil
     ##STR23##                 Slightly yellow oil
     ##STR24##                 m.p. 96-97.degree. C.
     ##STR25##                 Slightly yellow oil
     ##STR26##                 Slightly yellow oil
     ##STR27##                 Slightly yellow oil
     ##STR28##                 Slightly yellow oil
     ##STR29##                 Slightly yellow oil
     ##STR30##                 Slightly yellow oil
     ##STR31##                 Slightly yellow oil
     ##STR32##                 Slightly yellow oil
     ##STR33##                 Slightly yellow oil
     ##STR34##                 Slightly yellow oil
     ##STR35##                 Slightly yellow oil
     ##STR36##                 Slightly yellow oil
     ##STR37##                 Slightly yellow oil
     ##STR38##                 Slightly yellow oil
     ##STR39##                 Slightly yellow oil
     ##STR40##                 Slightly yellow oil
     ##STR41##                 Slightly yellow oil
     ##STR42##                 Slightly yellow oil
     ##STR43##                 Slightly yellow oil
     ##STR44##                 Slightly yellow oil
     ##STR45##                 Slightly yellow oil
     ##STR46##                 Slightly yellow oil
     ##STR47##                 m.p. 137.about. 139.degree. C.
     ##STR48##                 Slightly yellow oil
     ##STR49##                 Slightly yellow oil
     ##STR50##                 Slightly yellow oil
     ##STR51##                 Slightly yellow oil
     ##STR52##                 Slightly yellow oil
     ##STR53##                 Slightly yellow oil
     ##STR54##                 Slightly yellow oil
     ##STR55##                 Slightly yellow oil
     ##STR56##                 Slightly yellow oil
     ##STR57##                 Slightly yellow oil
     ##STR58##                 Slightly yellow oil
     ##STR59##                 Slightly yellow oil
     ##STR60##                 Slightly yellow oil
     ##STR61##                 Slightly yellow oil
     ##STR62##                 Slightly yellow oil
     ##STR63##                 Slightly yellow oil
     ##STR64##                 Slightly yellow oil
     ##STR65##                 Slightly yellow oil
     ##STR66##                 Slightly yellow oil
     ##STR67##                 Slightly yellow oil
     ##STR68##                 Slightly yellow oil
     ##STR69##                 Slightly yellow oil
     ##STR70##                 Slightly yellow oil
     ##STR71##                 Slightly yellow oil
     ##STR72##                 Slightly yellow oil
     ##STR73##                 Slightly yellow oil
     ##STR74##                 Slightly yellow oil
     ##STR75##                 Slightly yellow oil
     ##STR76##                 Slightly yellow oil
     ##STR77##                 Slightly yellow oil
     ##STR78##                 Slightly yellow oil
     ##STR79##                 m.p. 139.about. 140.degree. C.
     ##STR80##                 Slightly yellow oil
     ##STR81##                 Slightly yellow oil
     ##STR82##                 m.p. 144.about. 145.degree. C.
     ##STR83##                 m.p. 142.about. 143.degree. C.
     ##STR84##                 Slightly yellow oil
     ##STR85##                 Slightly yellow oil
     ##STR86##                 m.p. 160.about. 161.degree. C.
     ##STR87##                 Slightly yellow oil
    ______________________________________
     m.p.: melting point


REFERENCE EXAMPLE 5

Preparation of 3-methyl-5-phenyl-2-pyrazoline ##STR88##

17.1 g (342 mmol) of hydrazine monohydrate was dissolved in 500 ml of methanol. Then, 50 g (342 mmol) of trans-4-phenyl-3-buten-2-one dissolved in 100 ml of methanol was gradually dropwise added thereto under stirring within a range of from 5.degree. C. to 15.degree. C. Then, the mixture was stirred at room temperature for 30 hours, and methanol was distilled off under reduced pressure. The residue was distilled under reduced pressure to obtain 41.0 g of the desired 3-methyl-5-phenyl-2-pyrazoline.

Boiling point: 113.degree.-115.degree. C./0.2 mmHg.

The structural formulas and the physical properties or characteristics of the pyrazoline derivatives (3) prepared in the same manner as in Reference Example 5 are shown below:

    ______________________________________
     ##STR89##
     ##STR90##
     ##STR91##
     ##STR92##
     ##STR93##
     ##STR94##
     ##STR95##
     ##STR96##
     ##STR97##
     ##STR98##
     ##STR99##
     ##STR100##
     ##STR101##
     ##STR102##
     ##STR103##
     ##STR104##
     ##STR105##
     ##STR106##
     ##STR107##
     ##STR108##
     ##STR109##
     ##STR110##
     ##STR111##
     ##STR112##
     ##STR113##
     ##STR114##
     ##STR115##
     ##STR116##
     ##STR117##
     ##STR118##
     ##STR119##
     ##STR120##
     ##STR121##
     ##STR122##
     ##STR123##
     ##STR124##
     ##STR125##
     ##STR126##
     ##STR127##
     ##STR128##
     ##STR129##
     ##STR130##
     ##STR131##
     ##STR132##
     ##STR133##
     ##STR134##
     ##STR135##
     ##STR136##
    ______________________________________
     b.p.: boiling point


EXAMPLE 1

Preparation of 1-[(N-dimethylsulfamoyl-N-ethylamino)sulfonylcarbamoyl]-3-methyl-5-phenyl- 2-pyrazoline ##STR137##

A mixture comprising 3.3 g (9.4 mmol) of phenyl N-(N-dimethylsulfamoyl-N-ethylamino)sulfonyl]carbamate, 3.76 g (23.5 mmol) of 3-methyl-5-phenyl-2-pyrazoline and 30 ml of dry benzene was refluxed for 5 minutes. The mixture was left to cool, and then 50 ml of benzene was added thereto. The benzene layer was washed twice with dilute hydrochloric acid and then twice with water. Then, it was dried over anhydrous sodium sulfate. Thereafter, the solvent was distilled off under reduced pressure. The obtained residue was purified by silica gel column chromatography (CHCl.sub.3) and then washed sequentially with n-hexane and diethyl ether to obtain 2 g of the desired 1-[(N-dimethylsulfamoyl-N-ethylamino)sulfonylcarbamoyl]-3-methyl-5-phenyl- 2-pyrazoline.

Melting point: 138.degree.-139.degree. C.

EXAMPLE 2

Preparation of 1-[(N-dimethylsulfamoyl-N-methylamino)sulfonylcarbamoyl]-3-methyl-5-(2-thi enyl)-2-pyrazoline ##STR138##

A mixture comprising 1.69 g (5.0 mmol) of phenyl N-[(N-dimethylsulfamoyl-N-methylamino)sulfonyl]carbamate, 0.58 g (3.5 mmol) of 3-methyl-5-(2-thienyl)-2-pyrazoline and 10 ml of dry benzene, was refluxed for 10 minutes. The mixture was left to cool, and then benzene was distilled off under reduced pressure. The obtained residue was washed with n-hexane. Then, the residue was stirred together with diethyl ether. The precipitated crystalline product was isolated by suction filtration and then washed with diethyl ether to obtain 1.1 g of the desired 1-[(N-dimethylsulfamoyl-N-methylamino)sulfonylcarbamoyl]-3-methyl-5-(2-thi enyl)-2-pyrazoline.

Melting point: 112.degree.-113.degree. C.

EXAMPLE 3

Preparation of 1-[(N-dimethylsulfamoyl-N-methoxyamino)sulfonylcarbamoyl]-3-methyl-5-pheny l-2-pyrazoline ##STR139##

4.24 g (12 mmol) of phenyl N-[(N-dimethylsulfamoyl-N-methoxyamino)sulfonyl]carbamate was dissolved in 30 ml of dry benzene, and 1.6 g (10 mmol) of 3-methyl-5-phenyl-2-pyrazoline was added thereto. The mixture was refluxed for 5 minutes. The mixture was left to cool, and the solvent was distilled off under reduced pressure. The residue was purified by reverse phase column chromatography (CH.sub.3 CN: H.sub.2 O=7:3) to obtain 1.0 g of the desired 1-[(N-dimethylsulfamoyl-N-methoxyamino)sulfonylcarbamoyl]-3-methyl-5-pheny l-2-pyrazoline.

Melting point: 104.degree.-105.degree. C.

EXAMPLE 4

Preparation of 1-[(N-(N-methyl-N-methoxyaminosulfonyl)-N-methylamino)sulfonylcarbamoyl]-3 -methyl-5-phenyl-2-pyrazoline ##STR140##

A mixture comprising 1 g (2.83 mmol) of phenyl N-[(N-(N-methyl-N-methoxyaminosulfonyl)-N-methylamino)sulfonyl]-carbamate, 0.45 g (2.81 mmol) of 3-methyl-5-phenyl-2-pyrazoline and 30 ml of dry benzene was heated at 80.degree. C. for 5 minutes. The mixture was left to cool, and then the solvent was distilled off under reduced pressure. The residue was purified by reverse phase column chromatography (CH.sub.3 CN: H.sub.2 O=7:3) to obtain 0.5 g of the desired 1-[(N-(N-methyl-N-methoxyaminosulfonyl)-N-methyl-amino)sulfonylcarbamoyl]- 3-methyl-5-phenyl-2-pyrazoline as glassy substance.

EXAMPLE 5

Preparation of 1-(2-methyl-tetrahydro-1,2,6-thiadiazine-1,1-dioxide-6-sulfonylcarbamoyl)- 3-methyl-5-phenyl-2-pyrazoline ##STR141##

A mixture comprising 0.70 g (2 mmol) of phenyl N-(2-methyl-tetrahydro-1,2,6-thiadiazine-1,1-dioxide-6-sulfonyl)carbamate, 0.80 g (5 mmol) of 3-methyl-5-phenyl-2-pyrazoline and 30 ml of dry benzene, was refluxed for 5 minutes. The mixture was left to cool, and then 50 ml of benzene was added thereto. The benzene layer was washed three times with dilute hydrochloric acid and twice with water. Then, it was dried over anhydrous sodium sulfate, and then solvent was distilled off under reduced pressure. The obtained residue was washed sequentially with n-hexane and diethyl ether to obtain 0.7 g of the desired 1-(2-methyl-tetrahydro-1,2,6-thiadiazine-1,1- dioxide-6-sulfonylcarbamoyl)-3-methyl-5-phenyl-2-pyrazoline.

Melting point: 147.degree.-148.degree. C.

EXAMPLE 6

Preparation of 1-(2-methyl-tetrahydro-1,2,6-thiadiazine- 1,1-dioxide-6-sulfonylcarbamoyl)-3,5-dimethyl-5-phenyl-2-pyrazoline ##STR142##

A mixture comprising 8 g (22.9 mmol) of phenyl N-(2-methyl-tetrahydro-1,2,6-thiadiazine-1,1-dioxide-6-sulfonyl)carbamate, 5.1 g (29.3 mmol) of 3,5-dimethyl-5-phenyl-2-pyrazoline and 200 ml of dry benzene, was heated at 80.degree. C. for 5 minutes. The mixture was left to cool, and then solvent was distilled off under reduced pressure. The residue was washed with diethyl ether to obtain 6.2 g of the desired 1-(2-methyl-tetrahydro-1,2,6-thiadiazine-1,1-dioxide-6-sulfonylcarbamoyl)- 3,5-dimethyl-5-phenyl-2-pyrazoline.

Melting point: 151.degree.-154.degree. C.

The structural formulas and the physical properties or characteristics of the compounds prepared in the same manner as in Examples 1 to 6 are shown below: ##STR143##

Examples of compounds covered by the present invention including those prepared in the preceding Examples will be given in the following Tables 1 to 14 and Tables 1A to 14A. However, it should be understood that the compounds of the present invention are not limited to such specific Examples.

The symbols in the Tables have the following meanings.

Me: methyl group, Et: ethyl group, Pr-n: n-propyl group, Pr-i: isopropyl group, cyc-Pr: cyclopropyl group, Bu-n: n-butyl group, Bu-i: isobutyl group, Bu-sec: secondary butyl group, Bu-t: tert-butyl group, cyc-Bu: cyclobutyl group, Pen-n: n-pentyl group, cyc-Hex: cyclohexyl group, Ph: phenyl group, Gn is the same as the above G, and Ga, Gb and Gc have the following meanings.

Ga=G1-G643 (i.e. it means any one of G1 to G643.)

Gb=G1 -G72 and G102-G136 (i.e. it means any one of G1 to G72 and G102 to G136 .)

Gc=G1 -G35 and G102 -G136 (i.e. it means any one of G1 to G35 and G102 to G136 .) ##STR144##

                  TABLE 1
    ______________________________________
    R.sup.11    R.sup.12     R.sup.13    Gn
    ______________________________________
    H           Me           Me          Ga
    H           Me           Et          Ga
    H           Me           Ph          Ga
    H           Me           PhCH.sub.2  Ga
    H           Et           Et          Ga
    H           Pr-n         Pr-n        Gb
    H           (CH.sub.2).sub.4     Ga
    H           (CH.sub.2).sub.5     Ga
    Me          H            Me          Gc
    Me          H            Et          Gc
    Me          Me           Me          Ga
    Me          Me           Et          Ga
    Me          Me           Pr-n        Gb
    Me          Me           Pr-i        Gb
    Me          Me           Bu-n        Gb
    Me          Me           Ph          Ga
    Me          Me           Ph-2-Cl     Gb
    Me          Me           Ph-2-CO.sub.2 Me
                                         Gb
    Me          Me           Ph-2-OMe    Gb
    Me          Me           Ph-2-CF.sub.3
                                         Gb
    Me          Me           Ph-2-NO.sub.2
                                         Gb
    Me          Me           Ph-2-Me     Gb
    Me          Me           PhCH.sub.2  Ga
    Me          Et           Et          Ga
    Me          Pr-n         Pr-n        Gb
    Me          (CH.sub.2).sub.4     Ga
    Me          (CH.sub.2).sub.5     Ga
    Et          H            Me          Gc
    Et          H            Et          Gc
    Et          Me           Me          Ga
    Et          Me           Et          Ga
    Et          Me           Pr-n        Gb
    Et          Me           Pr-i        Gb
    Et          Me           Bu-n        Gb
    Et          Me           Ph          Ga
    Et          Me           Ph-2-Cl     Gb
    Et          Me           Ph-2-CO.sub.2 Me
                                         Gb
    Et          Me           Ph-2-OMe    Gb
    Et          Me           Ph-2-CF.sub.3
                                         Gb
    Et          Me           Ph-2-NO.sub.2
                                         Gb
    Et          Me           Ph-2-Me     Gb
    Et          Me           PhCH.sub.2  Ga
    Et          Et           Et          Ga
    Et          Pr-n         Pr-n        Gb
    Et          (CH.sub.2).sub.4     Ga
    Et          (CH.sub.2).sub.5     Ga
    Pr-n        H            Me          Gc
    Pr-n        H            Et          Gc
    Pr-n        Me           Me          Ga
    Pr-n        Me           Et          Ga
    Pr-n        Me           Pr-n        Gb
    Pr-n        Me           Pr-i        Gb
    Pr-n        Me           Bu-n        Gb
    Pr-n        Me           Ph          Ga
    Pr-n        Me           Ph-2-Cl     Gb
    Pr-n        Me           Ph-2-CO.sub.2 Me
                                         Gb
    Pr-n        Me           Ph-2-OMe    Gb
    Pr-n        Me           Ph-2-CF.sub.3
                                         Gb
    Pr-n        Me           Ph-2-NO.sub.2
                                         Gb
    Pr-n        Me           Ph-2-Me     Gb
    Pr-n        Me           PhCH.sub.2  Ga
    Pr-n        Et           Et          Ga
    Pr-n        Pr-n         Pr-n        Gb
    Pr-n        (CH.sub.2).sub.4     Ga
    Pr-n        (CH.sub.2).sub.5     Ga
    Pr-i        H            Me          Gc
    Pr-i        H            Et          Gc
    Pr-i        Me           Me          Ga
    Pr-i        Me           Et          Ga
    Pr-i        Me           Pr-n        Gb
    Pr-i        Me           Pr-i        Gb
    Pr-i        Me           Bu-n        Gb
    Pr-i        Me           Ph          Ga
    Pr-i        Me           Ph-2-Cl     Gb
    Pr-i        Me           Ph-2-CO.sub.2 Me
                                         Gb
    Pr-i        Me           Ph-2-OMe    Gb
    Pr-i        Me           Ph-2-CF.sub.3
                                         Gb
    Pr-i        Me           Ph-2-NO.sub.2
                                         Gb
    Pr-i        Me           Ph-2-Me     Gb
    Pr-i        Me           PhCH.sub.2  Ga
    Pr-i        Et           Et          Ga
    Pr-i        Pr-n         Pr-n        Gb
    Pr-i        (CH.sub.2).sub.4     Ga
    Pr-i        (CH.sub.2).sub.5     Ga
    cyc-Pr      Me           Me          Ga
    cyc-Pr      Me           Et          Ga
    cyc-Pr      Me           Ph          Ga
    cyc-Pr      Me           PhCH.sub.2  Ga
    cyc-Pr      Et           Et          Ga
    cyc-Pr      Pr-n         Pr-n        Gb
    cyc-Pr      (CH.sub.2).sub.4     Ga
    cyc-Pr      (CH.sub.2).sub.5     Ga
    cyc-PrCH.sub.2
                Me           Me          Ga
    cyc-PrCH.sub.2
                Me           Et          Ga
    cyc-PrCH.sub.2
                Me           Ph          Ga
    cyc-PrCH.sub.2
                Me           PhCH.sub.2  Ga
    cyc-PrCH.sub.2
                Et           Et          Ga
    cyc-PrCH.sub.2
                Pr-n         Pr-n        Gb
    cyc-PrCH.sub.2
                (CH.sub.2).sub.4     Ga
    cyc-PrCH.sub.2
                (CH.sub.2).sub.5     Ga
    Bu-n        H            Me           Gc
    Bu-n        H            Et          Gc
    Bu-n        Me           Me          Ga
    Bu-n        Me           Et          Ga
    Bu-n        Me           Pr-n        Gb
    Bu-n        Me           Pr-i        Gb
    Bu-n        Me           Bu-n        Gb
    Bu-n        Me           Ph          Ga
    Bu-n        Me           Ph-2-Cl     Gb
    Bu-n        Me           Ph-2-CO.sub.2 Me
                                         Gb
    Bu-n        Me           Ph-2-OMe    Gb
    Bu-n        Me           Ph-2-CF.sub.3
                                         Gb
    Bu-n        Me           Ph-2-NO.sub.2
                                         Gb
    Bu-n        Me           Ph-2-Me     Gb
    Bu-n        Me           PhCH.sub.2  Ga
    Bu-n        Et           Et          Ga
    Bu-n        Pr-n         Pr-n        Gb
    Bu-n        (CH.sub.2).sub.4     Ga
    Bu-n        (CH.sub.2).sub.5     Ga
    Bu-sec      H            Me          Gc
    Bu-sec      H            Et          Gc
    Bu-sec      Me           Me          Ga
    Bu-sec      Me           Et          Ga
    Bu-sec      Me           Ph          Ga
    Bu-sec      Me           PhCH.sub.2  Ga
    Bu-sec      Et           Et          Ga
    Bu-sec      Pr-n         Pr-n        Gb
    Bu-sec      (CH.sub.2).sub.4     Ga
    Bu-sec      (CH.sub.2).sub.5     Ga
    Bu-t        H            Me          Gc
    Bu-t        H            Et          Gc
    Bu-t        Me           Me          Ga
    Bu-t        Me           Et          Ga
    Bu-t        Me           Ph          Ga
    Bu-t        Me           PhCH.sub.2  Ga
    Bu-t        Et           Et          Ga
    Bu-t        Pr-n         Pr-n        Gb
    Bu-t        (CH.sub.2).sub.4     Ga
    Bu-t        (CH.sub.2 ).sub.5    Ga
    CH.sub.2CHCH.sub.2
                H            Me          Gc
    CH.sub.2CHCH.sub.2
                H            Et          Gc
    CH.sub.2CHCH.sub.2
                Me           Me          Ga
    CH.sub.2CHCH.sub.2
                Me           Et          Ga
    CH.sub.2CHCH.sub.2
                Me           Pr-n        Gb
    CH.sub.2CHCH.sub.2
                Me           Pr-i        Gb
    CH.sub.2CHCH.sub.2
                Me           Bu-n        Gb
    CH.sub.2CHCH.sub.2
                Me           Ph          Ga
    CH.sub.2CHCH.sub.2
                Me           Ph-2-Cl     Gb
    CH.sub.2CHCH.sub.2
                Me           Ph-2-CO.sub.2 Me
                                         Gb
    CH.sub.2CHCH.sub.2
                Me           Ph-2-OMe    Gb
    CH.sub.2CHCH.sub.2
                Me           Ph-2-CF.sub.3
                                         Gb
    CH.sub.2CHCH.sub.2
                Me           Ph-2-NO.sub.2
                                         Gb
    CH.sub.2CHCH.sub.2
                Me           Ph-2-Me     Gb
    CH.sub.2CHCH.sub.2
                Me           PhCH.sub.2  Ga
    CH.sub.2CHCH.sub.2
                Et           Et          Ga
    CH.sub.2CHCH.sub.2
                Pr-n         Pr-n        Gb
    CH.sub.2CHCH.sub.2
                (CH.sub.2).sub.4     Ga
    CH.sub.2CHCH.sub.2
                (CH.sub.2).sub.5     Ga
    CH CCH.sub.2
                H            Me          Gc
    CH CCH.sub.2
                H            Et          Gc
    CH  CCH.sub.2
                Me           Me          Ga
    CH CCH.sub.2
                Me           Et          Ga
    CH CCH.sub.2
                Me           Pr-n        Gb
    CH CCH.sub.2
                Me           Pr-i        Gb
    CH CCH.sub.2
                Me           Bu-n        Gb
    CH CCH.sub.2
                Me           Ph          Ga
    CH CCH.sub.2
                Me           Ph-2-Cl     Gb
    CH CCH.sub.2
                Me           Ph-2-CO.sub.2 Me
                                         Gb
    CH CCH.sub.2
                Me           Ph-2-OMe    Gb
    CH CCH.sub.2
                Me           Ph-2-CF.sub.3
                                         Gb
    CH CCH.sub.2
                Me           Ph-2-NO.sub.2
                                         Gb
    CH CCH.sub.2
                Me           Ph-2-Me     Gb
    CH CCH.sub.2
                Me           PhCH.sub.2  Ga
    CH  CCH.sub.2
                Et           Et          Ga
    CH CCH.sub.2
                Pr-n         Pr-n        Gb
    CH CCH.sub.2
                (CH.sub.2).sub.4     Ga
    CH CCH.sub.2
                (CH.sub.2).sub.5     Ga
    MeOCH.sub.2 Me           Me          Ga
    MeOCH.sub.2 Me           Et          Ga
    MeOCH.sub.2 Me           Ph          Ga
    MeOCH.sub.2 Me           PhCH.sub.2  Ga
    MeOCH.sub.2 Et           Et          Ga
    MeOCH.sub.2 Pr-n         Pr-n        Gb
    MeOCH.sub.2 (CH.sub.2).sub.4     Ga
    MeOCH.sub.2 (CH.sub.2).sub.5     Ga


EtOCH.sub.2 Me Me Ga EtOCH.sub.2 Me Et Ga EtOCH.sub.2 Me Ph Ga EtOCH.sub.2 Me PhCH.sub.2 Ga EtOCH.sub.2 Et Et Ga EtOCH.sub.2 Pr-n Pr-n Gb EtOCH.sub.2 (CH.sub.2).sub.4 Ga EtOCH.sub.2 (CH.sub.2).sub.5 Ga MeOCH.sub.2 CH.sub.2 H Me Gc MeOCH.sub.2 CH.sub.2 H Et Gc MeOCH.sub.2 CH.sub.2 Me Me Ga MeOCH.sub.2 CH.sub.2 Me Et Ga MeOCH.sub.2 CH.sub.2 Me Pr-n Gb MeOCH.sub.2 CH.sub.2 Me Pr-i Gb MeOCH.sub.2 CH.sub.2 Me Bu-n Gb MeOCH.sub.2 CH.sub.2 Me Ph Ga MeOCH.sub.2 CH.sub.2 Me Ph-2-Cl Gb MeOCH.sub.2 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb MeOCH.sub.2 CH.sub.2 Me Ph-2-OMe Gb MeOCH.sub.2 CH.sub.2 Me Ph-2-CF.sub.3 Gb MeOCH.sub.2 CH.sub.2 Me Ph-2-NO.sub.2 Gb MeOCH.sub.2 CH.sub.2 Me Ph-2-Me Gb MeOCH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga MeOCH.sub.2 CH.sub.2 Et Et Ga MeOCH.sub.2 CH.sub.2 Pr-n Pr-n Gb MeOCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga MeOCH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga EtOCH.sub.2 CH.sub.2 H Me Gc EtOCH.sub.2 CH.sub.2 H Et Gc EtOCH.sub.2 CH.sub.2 Me Me Ga EtOCH.sub.2 CH.sub.2 Me Et Ga EtOCH.sub.2 CH.sub.2 Me Pr-n Gb EtOCH.sub.2 CH.sub.2 Me Pr-i Gb EtOCH.sub.2 CH.sub.2 Me Bu-n Gb EtOCH.sub.2 CH.sub.2 Me Ph Ga EtOCH.sub.2 CH.sub.2 Me Ph-2-Cl Gb EtOCH.sub.2 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb EtOCH.sub.2 CH.sub.2 Me Ph-2-OMe Gb EtOCH.sub.2 CH.sub.2 Me Ph-2-CF.sub.3 Gb EtOCH.sub.2 CH.sub.2 Me Ph-2-NO.sub.2 Gb EtOCH.sub.2 CH.sub.2 Me Ph-2-Me Gb EtOCH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga EtOCH.sub.2 CH.sub.2 Et Et Ga EtOCH.sub.2 CH.sub.2 Pr-n Pr-n Gb EtOCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga EtOCH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga MeOCH.sub.2 (CH.sub.3)CH H Me Gc MeOCH.sub.2 (CH.sub.3)CH H Et Gc MeOCH.sub.2 (CH.sub.3)CH Me Me Ga MeOCH.sub.2 (CH.sub.3)CH Me Et Ga MeOCH.sub.2 (CH.sub.3)CH Me Pr-n Gb MeOCH.sub.2 (CH.sub.3)CH Me Pr-i Gb MeOCH.sub.2 (CH.sub.3)CH Me Bu-n Gb MeOCH.sub.2 (CH.sub.3)CH Me Ph Ga MeOCH.sub.2 (CH.sub.3)CH Me Ph-2-Cl Gb MeOCH.sub.2 (CH.sub.3)CH Me Ph-2-CO.sub.2 Me Gb MeOCH.sub.2 (CH.sub.3)CH Me Ph-2-OMe Gb MeOCH.sub.2 (CH.sub.3)CH Me Ph-2-CF.sub.3 Gb MeOCH.sub.2 (CH.sub.3)CH Me Ph-2-NO.sub.2 Gb MeOCH.sub.2 (CH.sub. 3)CH Me Ph-2-Me Gb MeOCH.sub.2 (CH.sub.3)CH Me PhCH.sub.2 Ga MeOCH.sub.2 (CH.sub.3)CH Et Et Ga MeOCH.sub.2 (CH.sub.3)CH Pr-n Pr-n Gb MeOCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.4 Ga MeOCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.5 Ga EtOCH.sub.2 (CH.sub.3)CH H Me Gc EtOCH.sub.2 (CH.sub.3)CH H Et Gc EtOCH.sub.2 (CH.sub.3)CH Me Me Ga EtOCH.sub.2 (CH.sub.3)CH Me Et Ga EtOCH.sub.2 (CH.sub.3)CH Me Pr-n Gb EtOCH.sub.2 (CH.sub.3)CH Me Pr-i Gb EtOCH.sub.2 (CH.sub.3)CH Me Bu-n Gb EtOCH.sub.2 (CH.sub.3)CH Me Ph Ga EtOCH.sub.2 (CH.sub.3)CH Me Ph-2-Cl Gb EtOCH.sub.2 (CH.sub.3)CH Me Ph-2-CO.sub.2 Me Gb EtOCH.sub.2 (CH.sub.3)CH Me Ph-2-OMe Gb EtOCH.sub.2 (CH.sub.3)CH Me Ph-2-CF.sub.3 Gb EtOCH.sub.2 (CH.sub.3)CH Me Ph-2-NO.sub.2 Gb EtOCH.sub.2 (CH.sub.3)CH Me Ph-2-Me Gb EtOCH.sub.2 (CH.sub.3)CH Me PhCH.sub.2 Ga EtOCH.sub.2 (CH.sub.3)CH Et Et Ga EtOCH.sub.2 (CH.sub.3 )CH Pr-n Pr-n Gb EtOCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.4 Ga EtOCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.5 Ga CHF.sub.2 OCH.sub.2 H Me Gc CHF.sub.2 OCH.sub.2 H Et Gc CHF.sub.2 OCH.sub.2 Me Me Ga CHF.sub.2 OCH.sub.2 Me Et Ga CHF.sub.2 OCH.sub.2 Me Pr-n Gb CHF.sub.2 OCH.sub.2 Me Pr-i Gb CHF.sub.2 OCH.sub.2 Me Bu-n Gb CHF.sub.2 OCH.sub.2 Me Ph Ga CHF.sub.2 OCH.sub.2 Me Ph-2-Cl Gb CHF.sub.2 OCH.sub.2 Me Ph-2-CO.sub.2 Me Gb CHF.sub.2 OCH.sub.2 Me Ph-2-OMe Gb CHF.sub.2 OCH.sub.2 Me Ph-2-CF.sub.3 Gb CHF.sub.2 OCH.sub.2 Me Ph-2-NO.sub.2 Gb CHF.sub.2 OCH.sub.2 Me Ph-2-Me Gb CHF.sub.2 OCH.sub.2 Me PhCH.sub.2 Ga CHF.sub.2 OCH.sub.2 Et Et Ga CHF.sub.2 OCH.sub.2 Pr-n Pr-n Gb CHF.sub.2 OCH.sub.2 (CH.sub.2).sub.4 Ga CHF.sub.2 OCH.sub.2 (CH.sub.2).sub.5 Ga MeSCH.sub.2 Me Me Ga MeSCH.sub.2 Me Et Ga MeSCH.sub. 2 Me Ph Ga MeSCH.sub.2 Me PhCH.sub.2 Ga MeSCH.sub.2 Et Et Ga MeSCH.sub.2 Pr-n Pr-n Gb MeSCH.sub.2 (CH.sub.2).sub.4 Ga MeSCH.sub.2 (CH.sub.2).sub.5 Ga EtSCH.sub.2 Me Me Ga EtSCH.sub.2 Me Et Ga EtSCH.sub.2 Me Ph Ga EtSCH.sub.2 Me PhCH.sub.2 Ga EtSCH.sub.2 Et Et Ga EtSCH.sub.2 Pr-n Pr-n Gb EtSCH.sub.2 (CH.sub.2).sub.4 Ga EtSCH.sub.2 (CH.sub.2).sub.5 Ga MeSCH.sub.2 CH.sub.2 H Me Gc MeSCH.sub.2 CH.sub.2 H Et Gc MeSCH.sub.2 CH.sub.2 Me Me Ga MeSCH.sub.2 CH.sub.2 Me Et Ga MeSCH.sub.2 CH.sub.2 Me Pr-n Gb MeSCH.sub.2 CH.sub.2 Me Pr-i Gb MeSCH.sub.2 CH.sub.2 Me Bu-n Gb MeSCH.sub.2 CH.sub.2 Me Ph Ga MeSCH.sub.2 CH.sub.2 Me Ph-2-Cl Gb MeSCH.sub.2 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb MeSCH.sub.2 CH.sub.2 Me Ph-2-OMe Gb

MeSCH.sub.2 CH.sub.2 Me Ph-2-CF.sub.3 Gb MeSCH.sub.2 CH.sub.2 Me Ph-2-NO.sub.2 Gb MeSCH.sub.2 CH.sub. 2 Me Ph-2-Me Gb MeSCH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga MeSCH.sub.2 CH.sub.2 Et Et Ga MeSCH.sub.2 CH.sub.2 Pr-n Pr-n Gb MeSCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga MeSCH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga EtSCH.sub.2 CH.sub.2 H Me Gc EtSCH.sub.2 CH.sub.2 H Et Gc EtSCH.sub.2 CH.sub.2 Me Me Ga EtSCH.sub.2 CH.sub.2 Me Et Ga EtSCH.sub.2 CH.sub.2 Me Pr-n Gb EtSCH.sub.2 CH.sub.2 Me Pr-i Gb EtSCH.sub.2 CH.sub.2 Me Bu-n Gb EtSCH.sub.2 CH.sub.2 Me Ph Ga EtSCH.sub.2 CH.sub.2 Me Ph-2-Cl Gb EtSCH.sub.2 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb EtSCH.sub.2 CH.sub.2 Me Ph-2-OMe Gb EtSCH.sub.2 CH.sub.2 Me Ph-2-CF.sub.3 Gb EtSCH.sub.2 CH.sub.2 Me Ph-2-NO.sub.2 Gb EtSCH.sub.2 CH.sub.2 Me Ph-2-Me Gb EtSCH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga EtSCH.sub.2 CH.sub.2 Et Et Ga EtSCH.sub.2 CH.sub.2 Pr-n Pr-n Gb EtSCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga EtSCH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga MeSO.sub.2 CH.sub.2 Me Me Ga MeSO.sub.2 CH.sub.2 Me Et Ga MeSO.sub.2 CH.sub.2 Me Ph Ga MeSO.sub.2 CH.sub.2 Me PhCH.sub.2 Ga MeSO.sub.2 CH.sub.2 Et Et Ga MeSO.sub.2 CH.sub.2 Pr-n Pr-n Gb MeSO.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga MeSO.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga EtSO.sub.2 CH.sub.2 Me Me Ga EtSO.sub.2 CH.sub.2 Me Et Ga EtSO.sub.2 CH.sub.2 Me Ph Ga EtSO.sub.2 CH.sub.2 Me PhCH.sub.2 Ga EtSO.sub.2 CH.sub.2 Et Et Ga EtSO.sub.2 CH.sub.2 Pr-n Pr-n Gb EtSO.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga EtSO.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga MeSO.sub.2 CH.sub.2 CH.sub.2 H Me Gc MeSO.sub.2 CH.sub.2 CH.sub.2 H Et Gc MeSO.sub.2 CH.sub.2 CH.sub.2 Me Me Ga MeSO.sub.2 CH.sub.2 CH.sub.2 Me Et Ga MeSO.sub.2 CH.sub.2 CH.sub.2 Me Pr-n Gb MeSO.sub.2 CH.sub.2 CH.sub.2 Me Pr-i Gb MeSO.sub.2 CH.sub.2 CH.sub.2 Me Bu-n Gb MeSO.sub.2 CH.sub.2 CH.sub.2 Me Ph Ga MeSO.sub.2 CH.sub.2 CH.sub.2 Me Ph-2-Cl Gb MeSO.sub.2 CH.sub.2 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb MeSO.sub.2 CH.sub.2 CH.sub.2 Me Ph-2-OMe Gb MeSO.sub.2 CH.sub.2 CH.sub.2 Me Ph-2-CF.sub.3 Gb MeSO.sub.2 CH.sub.2 CH.sub.2 Me Ph-2-NO.sub.2 Gb MeSO.sub.2 CH.sub.2 CH.sub.2 Me Ph-2-Me Gb MeSO.sub.2 CH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga MeSO.sub.2 CH.sub.2 CH.sub.2 Et Et Ga MeSO.sub.2 CH.sub.2 CH.sub.2 Pr-n Pr-n Gb MeSO.sub.2 CH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga MeSO.sub.2 CH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga EtSO.sub.2 CH.sub.2 CH.sub.2 H Me Gc EtSO.sub.2 CH.sub.2 CH.sub.2 H Et Gc EtSO.sub.2 CH.sub.2 CH.sub.2 Me Me Ga EtSO.sub.2 CH.sub.2 CH.sub.2 Me Et Ga EtSO.sub.2 CH.sub.2 CH.sub.2 Me Pr-n Gb EtSO.sub.2 CH.sub.2 CH.sub.2 Me Pr-i Gb EtSO.sub.2 CH.sub.2 CH.sub.2 Me Bu-n Gb EtSO.sub.2 CH.sub.2 CH.sub.2 Me Ph Ga EtSO.sub.2 CH.sub.2 CH.sub.2 Me Ph-2-Cl Gb EtSO.sub.2 CH.sub.2 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb EtSO.sub.2 CH.sub.2 CH.sub.2 Me Ph-2-OMe Gb EtSO.sub.2 CH.sub.2 CH.sub.2 Me Ph-2-CF.sub.3 Gb EtSO.sub.2 CH.sub.2 CH.sub.2 Me Ph-2-NO.sub.2 Gb EtSO.sub.2 CH.sub.2 CH.sub.2 Me Ph-2-Me Gb EtSO.sub.2 CH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga EtSO.sub.2 CH.sub.2 CH.sub.2 Et Et Ga EtSO.sub.2 CH.sub.2 CH.sub.2 Pr-n Pr-n Gb EtSO.sub.2 CH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga EtSO.sub.2 CH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga FCH.sub.2 Me Me Ga FCH.sub.2 Me Et Ga FCH.sub.2 Me Ph Ga FCH.sub.2 Me PhCH.sub.2 Ga FCH.sub.2 Et Et Ga FCH.sub.2 Pr-n Pr-n Gb FCH.sub.2 (CH.sub.2).sub.4 Ga FCH.sub.2 (CH.sub.2).sub.5 Ga ClCH.sub.2 Me Me Ga ClCH.sub.2 Me Et Ga ClCH.sub.2 Me Ph Ga ClCH.sub.2 Me PhCH.sub.2 Ga ClCH.sub.2 Et Et Ga ClCH.sub.2 Pr-n Pr-n Gb ClCH.sub.2 (CH.sub.2).sub.4 Ga ClCH.sub.2 (CH.sub.2).sub.5 Ga BrCH.sub.2 Me Me Ga BrCH.sub.2 Me Et Ga BrCH.sub.2 Me Ph Ga BrCH.sub.2 Me PhCH.sub.2 Ga BrCH.sub.2 Et Et Ga BrCH.sub.2 Pr-n Pr-n Gb BrCH.sub.2 (CH.sub.2).sub.4 Ga BrCH.sub.2 (CH.sub.2).sub.5 Ga ICH.sub.2 Me Me Ga ICH.sub.2 Me Et Ga ICH.sub.2 Me Ph Ga ICH.sub.2 Me PhCH.sub.2 Ga ICH.sub.2 Et Et Ga ICH.sub.2 Pr-n Pr-n Gb ICH.sub.2 (CH.sub.2).sub.4 Ga ICH.sub.2 (CH.sub.2).sub.5 Ga FCH.sub.2 CH.sub.2 H Me Gc FCH.sub.2 CH.sub.2 H Et Gc FCH.sub.2 CH.sub.2 Me Me Ga FCH.sub.2 CH.sub.2 Me Et Ga FCH.sub.2 CH.sub.2 Me Pr-n Gb FCH.sub.2 CH.sub.2 Me Pr-i Gb FCH.sub.2 CH.sub.2 Me Bu-n Gb FCH.sub.2 CH.sub.2 Me Ph Ga FCH.sub.2 CH.sub.2 Me Ph-2-Cl Gb FCH.sub.2 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb FCH.sub.2 CH.sub.2 Me Ph-2-OMe Gb FCH.sub.2 CH.sub.2 Me Ph-2-CF.sub.3 Gb FCH.sub.2 CH.sub.2 Me Ph-2-NO.sub.2 Gb FCH.sub.2 CH.sub.2 Me Ph-2-Me Gb FCH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga FCH.sub.2 CH.sub.2 Et Et Ga FCH.sub.2 CH.sub.2 Pr-n Pr-n Gb FCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga FCH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga ClCH.sub.2 CH.sub.2 H Me Gc ClCH.sub.2 CH.sub.2 H Et Gc ClCH.sub.2 CH.sub.2 Me Me Ga ClCH.sub.2 CH.sub.2 Me Et Ga

ClCH.sub.2 CH.sub.2 Me Pr-n Gb ClCH.sub.2 CH.sub.2 Me Pr-i Gb ClCH.sub.2 CH.sub.2 Me Bu-n Gb ClCH.sub.2 CH.sub.2 Me Ph Ga ClCH.sub.2 CH.sub.2 Me Ph-2-Cl Gb ClCH.sub.2 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb ClCH.sub.2 CH.sub.2 Me Ph-2-OMe Gb ClCH.sub. 2 CH.sub.2 Me Ph-2-CF.sub.3 Gb ClCH.sub.2 CH.sub.2 Me Ph-2-NO.sub.2 Gb ClCH.sub.2 CH.sub.2 Me Ph-2-Me Gb ClCH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga ClCH.sub.2 CH.sub.2 Et Et Ga ClCH.sub.2 CH.sub.2 Pr-n Pr-n Gb ClCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga ClCH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga BrCH.sub.2 CH.sub.2 H Me Gc BrCH.sub.2 CH.sub.2 H Et Gc BrCH.sub.2 CH.sub.2 Me Me Ga BrCH.sub.2 CH.sub.2 Me Et Ga BrCH.sub.2 CH.sub.2 Me Pr-n Gb BrCH.sub.2 CH.sub.2 Me Pr-i Gb BrCH.sub.2 CH.sub.2 Me Bu-n Gb BrCH.sub.2 CH.sub.2 Me Ph Ga BrCH.sub.2 CH.sub.2 Me Ph-2-Cl Gb BrCH.sub.2 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb BrCH.sub.2 CH.sub.2 Me Ph-2-OMe Gb BrCH.sub.2 CH.sub.2 Me Ph-2-CF.sub.3 Gb BrCH.sub.2 CH.sub.2 Me Ph-2-NO.sub.2 Gb BrCH.sub.2 CH.sub.2 Me Ph-2-Me Gb BrCH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga BrCH.sub.2 CH.sub.2 Et Et Ga BrCH.sub.2 CH.sub.2 Pr-n Pr-n Gb BrCH.sub. 2 CH.sub.2 (CH.sub.2).sub.4 Ga BrCH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga ICH.sub.2 CH.sub.2 H Me Gc ICH.sub.2 CH.sub.2 H Et Gc ICH.sub.2 CH.sub.2 Me Me Ga ICH.sub.2 CH.sub.2 Me Et Ga ICH.sub.2 CH.sub.2 Me Pr-n Gb ICH.sub.2 CH.sub.2 Me Pr-i Gb ICH.sub.2 CH.sub.2 Me Bu-n Gb ICH.sub.2 CH.sub.2 Me Ph Ga ICH.sub.2 CH.sub.2 Me Ph-2-Cl Gb ICH.sub.2 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb ICH.sub.2 CH.sub.2 Me Ph-2-OMe Gb ICH.sub.2 CH.sub.2 Me Ph-2-CF.sub.3 Gb ICH.sub.2 CH.sub.2 Me Ph-2-NO.sub.2 Gb ICH.sub.2 CH.sub.2 Me Ph-2-Me Gb ICH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga ICH.sub.2 CH.sub.2 Et Et Ga ICH.sub.2 CH.sub.2 Pr-n Pr-n Gb ICH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga ICH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga FCH.sub.2 (CH.sub.3)CH Me Me Ga FCH.sub.2 (CH.sub.3)CH Me Et Ga FCH.sub.2 (CH.sub. 3)CH Me Ph Ga FCH.sub.2 (CH.sub.3)CH Me PhCH.sub.2 Ga FCH.sub.2 (CH.sub.3)CH Et Et Ga FCH.sub.2 (CH.sub.3)CH Pr-n Pr-n Gb FCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.4 Ga FCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.5 Ga ClCH.sub.2 (CH.sub.3)CH Me Me Ga ClCH.sub.2 (CH.sub.3)CH Me Et Ga ClCH.sub.2 (CH.sub.3)CH Me Ph Ga ClCH.sub.2 (CH.sub.3)CH Me PhCH.sub.2 Ga ClCH.sub.2 (CH.sub.3)CH Et Et Ga ClCH.sub.2 (CH.sub.3)CH Pr-n Pr-n Gb ClCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.4 Ga ClCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.5 Ga BrCH.sub.2 (CH.sub.3)CH Me Me Ga BrCH.sub.2 (CH.sub.3)CH Me Et Ga BrCH.sub.2 (CH.sub.3)CH Me Ph Ga BrCH.sub.2 (CH.sub.3)CH Me PhCH.sub.2 Ga BrCH.sub.2 (CH.sub.3)CH Et Et Ga BrCH.sub.2 (CH.sub.3)CH Pr-n Pr-n Gb BrCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.4 Ga BrCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.5 Ga ICH.sub.2 (CH.sub.3)CH Me Me Ga ICH.sub.2 (CH.sub.3)CH Me Et Ga ICH.sub.2 (CH.sub.3)CH Me Ph Ga ICH.sub.2 (CH.sub.3)CH Me PhCH.sub.2 Ga ICH.sub.2 (CH.sub.3)CH Et Et Ga ICH.sub.2 (CH.sub.3)CH Pr-n Pr-n Gb ICH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.4 Ga ICH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.5 Ga CF.sub.3 CH.sub.2 H Me Gc CF.sub.3 CH.sub.2 H Et Gc CF.sub.3 CH.sub.2 Me Me Ga CF.sub.3 CH.sub.2 Me Et Ga CF.sub.3 CH.sub.2 Me Pr-n Gb CF.sub.3 CH.sub.2 Me Pr-i Gb CF.sub.3 CH.sub.2 Me Bu-n Gb CF.sub.3 CH.sub.2 Me Ph Ga CF.sub.3 CH.sub.2 Me Ph-2-Cl Gb CF.sub.3 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb CF.sub.3 CH.sub.2 Me Ph-2-OMe Gb CF.sub.3 CH.sub.2 Me Ph-2-CF.sub.3 Gb CF.sub.3 CH.sub.2 Me Ph-2-NO.sub.2 Gb CF.sub.3 CH.sub.2 Me Ph-2-Me Gb CF.sub.3 CH.sub.2 Me PhCH.sub.2 Ga CF.sub.3 CH.sub.2 Et Et Ga CF.sub.3 CH.sub.2 Pr-n Pr-n Gb CF.sub.3 CH.sub.2 (CH.sub.2).sub.4 Ga CF.sub.3 CH.sub.2 (CH.sub.2).sub.5 Ga NCCH.sub.2 H Me Gc NCCH.sub.2 H Et Gc NCCH.sub.2 Me Me Ga NCCH.sub.2 Me Et Ga NCCH.sub.2 Me Pr-n Gb NCCH.sub.2 Me Pr-i Gb NCCH.sub.2 Me Bu-n Gb NCCH.sub.2 Me Ph Ga NCCH.sub.2 Me Ph-2-Cl Gb NCCH.sub.2 Me Ph-2-CO.sub.2 Me Gb NCCH.sub.2 Me Ph-2-OMe Gb NCCH.sub.2 Me Ph-2-CF.sub.3 Gb NCCH.sub.2 Me Ph-2-NO.sub.2 Gb NCCH.sub.2 Me Ph-2-Me Gb NCCH.sub.2 Me PhCH.sub.2 Ga NCCH.sub.2 Et Et Ga NCCH.sub.2 Pr-n Pr-n Gb NCCH.sub.2 (CH.sub.2).sub.4 Ga NCCH.sub.2 (CH.sub.2).sub.5 Ga NCCH.sub.2 CH.sub.2 H Me Gc NCCH.sub.2 CH.sub.2 H Et Gc NCCH.sub.2 CH.sub.2 Me Me Ga NCCH.sub.2 CH.sub.2 Me Et Ga NCCH.sub.2 CH.sub.2 Me Pr-n Gb

NCCH.sub.2 CH.sub.2 Me Pr-i Gb NCCH.sub.2 CH.sub.2 Me Bu-n Gb NCCH.sub.2 CH.sub.2 Me Ph Ga NCCH.sub.2 CH.sub.2 Me Ph-2-Cl Gb NCCH.sub.2 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb NCCH.sub.2 CH.sub.2 Me Ph-2-OMe Gb NCCH.sub.2 CH.sub.2 Me Ph-2-CF.sub.3 Gb NCCH.sub.2 CH.sub.2 Me Ph-2-NO.sub.2 Gb NCCH.sub.2 CH.sub.2 Me Ph-2-Me Gb NCCH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga NCCH.sub.2 CH.sub.2 Et Et Ga NCCH.sub.2 CH.sub.2 Pr-n Pr-n Gb NCCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga NCCH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga MeO.sub.2 CCH.sub.2 H Me Gc MeO.sub.2 CCH.sub.2 H Et Gc MeO.sub.2 CCH.sub.2 Me Me Ga MeO.sub.2 CCH.sub.2 Me Et Ga MeO.sub.2 CCH.sub.2 Me Pr-n Gb MeO.sub.2 CCH.sub.2 Me Pr-i Gb MeO.sub.2 CCH.sub.2 Me Bu-n Gb MeO.sub.2 CCH.sub.2 Me Ph Ga MeO.sub.2 CCH.sub.2 Me Ph-2-Cl Gb MeO.sub.2 CCH.sub.2 Me Ph-2-CO.sub.2 Me Gb MeO.sub.2 CCH.sub.2 Me Ph-2-OMe Gb MeO.sub.2 CCH.sub.2 Me Ph-2-CF.sub.3 Gb MeO.sub.2 CCH.sub.2 Me Ph-2-NO.sub.2 Gb MeO.sub.2 CCH.sub.2 Me Ph-2-Me Gb MeO.sub.2 CCH.sub.2 Me PhCH.sub.2 Ga MeO.sub.2 CCH.sub.2 Et Et Ga MeO.sub.2 CCH.sub.2 Pr-n Pr-n Gb MeO.sub.2 CCH.sub.2 (CH.sub.2).sub.4 Ga MeO.sub.2 CCH.sub.2 (CH.sub.2).sub.5 Ga EtO.sub.2 CCH.sub.2 H Me Gc EtO.sub.2 CCH.sub.2 H Et Gc EtO.sub.2 CCH.sub.2 Me Me Ga EtO.sub.2 CCH.sub.2 Me Et Ga EtO.sub.2 CCH.sub.2 Me Pr-n Gb EtO.sub.2 CCH.sub.2 Me Pr-i Gb EtO.sub.2 CCH.sub.2 Me Bu-n Gb EtO.sub.2 CCH.sub.2 Me Ph Ga EtO.sub.2 CCH.sub.2 Me Ph-2-Cl Gb EtO.sub.2 CCH.sub.2 Me Ph-2-CO.sub.2 Me Gb EtO.sub.2 CCH.sub.2 Me Ph-2-OMe Gb EtO.sub.2 CCH.sub.2 Me Ph-2-CF.sub.3 Gb EtO.sub.2 CCH.sub.2 Me Ph-2-NO.sub.2 Gb EtO.sub.2 CCH.sub.2 Me Ph-2-Me Gb EtO.sub.2 CCH.sub.2 Me PhCH.sub.2 Ga EtO.sub.2 CCH.sub.2 Et Et Ga EtO.sub.2 CCH.sub.2 Pr-n Pr-n Gb EtO.sub.2 CCH.sub.2 (CH.sub.2).sub.4 Ga EtO.sub.2 CCH.sub.2 (CH.sub.2).sub.5 Ga Pr-nO.sub.2 CCH.sub.2 Me Me Ga Pr-nO.sub.2 CCH.sub.2 Me Et Ga Pr-nO.sub.2 CCH.sub.2 Me Ph Ga Pr-nO.sub.2 CCH.sub.2 Me PhCH.sub.2 Ga Pr-nO.sub.2 CCH.sub.2 Et Et Ga Pr-nO.sub.2 CCH.sub.2 Pr-n Pr-n Gb Pr-nO.sub.2 CCH.sub.2 (CH.sub.2).sub.4 Ga Pr-nO.sub.2 CCH.sub.2 (CH.sub.2).sub.5 Ga MeO.sub.2 CCH.sub.2 CH.sub.2 H Me Gc MeO.sub.2 CCH.sub.2 CH.sub.2 H Et Gc MeO.sub.2 CCH.sub.2 CH.sub.2 Me Me Ga MeO.sub.2 CCH.sub.2 CH.sub.2 Me Et Ga MeO.sub.2 CCH.sub.2 CH.sub.2 Me Pr-n Gb MeO.sub.2 CCH.sub.2 CH.sub.2 Me Pr-i Gb MeO.sub.2 CCH.sub.2 CH.sub.2 Me Bu-n Gb MeO.sub.2 CCH.sub.2 CH.sub.2 Me Ph Ga MeO.sub.2 CCH.sub.2 CH.sub.2 Me Ph-2-Cl Gb MeO.sub.2 CCH.sub.2 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb MeO.sub.2 CCH.sub.2 CH.sub.2 Me Ph-2-OMe Gb MeO.sub.2 CCH.sub.2 CH.sub.2 Me Ph-2-CF.sub.3 Gb MeO.sub.2 CCH.sub.2 CH.sub.2 Me Ph-2-NO.sub.2 Gb MeO.sub.2 CCH.sub.2 CH.sub.2 Me Ph-2-Me Gb MeO.sub.2 CCH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga MeO.sub.2 CCH.sub.2 CH.sub.2 Et Et Ga MeO.sub.2 CCH.sub.2 CH.sub.2 Pr-n Pr-n Gb MeO.sub.2 CCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga MeO.sub.2 CCH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga EtO.sub.2 CCH.sub.2 CH.sub.2 H Me Gc EtO.sub.2 CCH.sub.2 CH.sub.2 H Et Gc EtO.sub.2 CCH.sub.2 CH.sub.2 Me Me Ga EtO.sub.2 CCH.sub.2 CH.sub.2 Me Et Ga EtO.sub.2 CCH.sub.2 CH.sub.2 Me Pr-n Gb EtO.sub.2 CCH.sub.2 CH.sub.2 Me Pr-i Gb EtO.sub.2 CCH.sub.2 CH.sub.2 Me Bu-n Gb EtO.sub.2 CCH.sub.2 CH.sub.2 Me Ph Ga EtO.sub.2 CCH.sub.2 CH.sub.2 Me Ph-2-Cl Gb EtO.sub.2 CCH.sub.2 CH.sub.2 Me Ph-2-CO.sub.2 Me Gb EtO.sub.2 CCH.sub.2 CH.sub.2 Me Ph-2-OMe Gb EtO.sub.2 CCH.sub.2 CH.sub.2 Me Ph-2-CF.sub.3 Gb EtO.sub.2 CCH.sub.2 CH.sub.2 Me Ph-2-NO.sub.2 Gb EtO.sub.2 CCH.sub.2 CH.sub.2 Me Ph-2-Me Gb EtO.sub.2 CCH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga EtO.sub.2 CCH.sub.2 CH.sub.2 Et Et Ga EtO.sub.2 CCH.sub.2 CH.sub.2 Pr-n Pr-n Gb EtO.sub.2 CCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga EtO.sub.2 CCH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga Pr-nO.sub.2 CCH.sub.2 CH.sub.2 Me Me Ga Pr-nO.sub.2 CCH.sub.2 CH.sub.2 Me Et Ga Pr-nO.sub.2 CCH.sub.2 CH.sub.2 Me Ph Ga Pr-nO.sub.2 CCH.sub.2 CH.sub.2 Me PhCH.sub.2 Ga Pr-nO.sub.2 CCH.sub.2 CH.sub.2 Et Et Ga Pr-nO.sub.2 CCH.sub.2 CH.sub.2 Pr-n Pr-n Gb Pr-nO.sub.2 CCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga Pr-nO.sub.2 CCH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Ga MeCOCH.sub.2 Me Me Ga MeCOCH.sub.2 Me Et Ga MeCOCH.sub.2 Me Ph Ga MeCOCH.sub.2 Me PhCH.sub.2 Ga MeCOCH.sub.2 Et Et Ga MeCOCH.sub.2 Pr-n Pr-n Gb MeCOCH.sub.2 (CH.sub.2).sub.4 Ga MeCOCH.sub.2 (CH.sub.2).sub.5 Ga EtCOCH.sub.2 Me Me Ga EtCOCH.sub.2 Me Et Ga EtCOCH.sub.2 Me Ph Ga EtCOCH.sub.2 Me PhCH.sub.2 Ga EtCOCH.sub.2 Et Et Ga EtCOCH.sub.2 Pr-n Pr-n Gb

EtCOCH.sub.2 (CH.sub.2).sub.4 Ga EtCOCH.sub.2 (CH.sub.2).sub.5 Ga PhCH.sub.2 H Me Gc PhCH.sub.2 H Et Gc PhCH.sub.2 Me Me Ga PhCH.sub.2 Me Et Ga PhCH.sub.2 Me Pr-n Gb PhCH.sub.2 Me Pr-i Gb PhCH.sub.2 Me Bu-n Gb PhCH.sub.2 Me Ph Ga PhCH.sub.2 Me Ph-2-Cl Gb PhCH.sub.2 Me Ph-2-CO.sub.2 Me Gb PhCH.sub.2 Me Ph-2-OMe Gb PhCH.sub.2 Me Ph-2-CF.sub.3 Gb PhCH.sub.2 Me Ph-2-NO.sub.2 Gb PhCH.sub.2 Me Ph-2-Me Gb PhCH.sub.2 Me PhCH.sub.2 Ga PhCH.sub.2 Et Et Ga PhCH.sub.2 Pr-n Pr-n Gb PhCH.sub.2 (CH.sub.2).sub.4 Ga PhCH.sub. 2 (CH.sub.2).sub.5 Ga Ph Me Me Ga Ph Me Et Ga Ph (CH.sub.2).sub.4 Ga Ph (CH.sub.2).sub.5 Ga Me CH.sub.2CHCH.sub.2 Me Ga Et CH.sub.2CHCH.sub.2 Me Ga Me CH CCH.sub.2 Me Ga Et CH CCH.sub.2 Me Ga Me CH.sub.2CHCH.sub.2 CH.sub.2CHCH.sub.2 Ga Et CH.sub.2CHCH.sub.2 CH.sub.2CHCH.sub.2 Ga Me CH CCH.sub.2 CH CCH.sub.2 Ga Et CH CCH.sub.2 CH CCH.sub.2 Ga Me H H Gb Et H H Gb Bu-i Me Me Gb cyc-Bu Me Me Gb cyc-Pen Me Me Gc cyc-Hex Me Me Gc Ph-2-Me Me Me Gb Ph-3-Me Me Me Gb Ph-4-OMe Me Me Gb Ph-3-OMe Me Me Gb Ph-2-OMe Me Me Gb Ph-4-Cl Me Me Gb Ph-3-Cl Me Me Gb Ph-2-Cl Me Me Gb Ph-2,6-Cl.sub.2 Me Me Gb ______________________________________

TABLE 2 ______________________________________ ##STR145## R.sup.11 R.sup.12 R.sup.13 Gn ______________________________________ Me H Me Gc Me H Et Gc Me Me Me Ga Me Me Et Ga Me Me Pr-n Gb Me Me Pr-i Gb Me Me Bu-n Gb Me Me Ph Ga Me Me Ph-2-Cl Gb Me Me Ph-2-CO.sub.2 Me Gb Me Me Ph-2-OMe Gb Me Me Ph-2-CF.sub.3 Gb Me Me Ph-2-NO.sub.2 Gb Me Me Ph-2-Me Gb Me Me Ph-CH.sub.2 Ga Me Et Et Ga Me Pr-n Pr-n Gb Me (CH.sub.2).sub.4 Ga Me (CH.sub.2).sub.5 Ga Et H Me Gc Et H Et Gc Et Me Me Ga Et Me Et Ga Et Me Pr-n Gb Et Me Pr-i Gb Et Me Bu-n Gb Et Me Ph Ga Et Me Ph-2-Cl Gb Et Me Ph-2-CO.sub.2 Me Gb Et Me Ph-2-OMe Gb Et Me Ph-2-CF.sub.3 Gb Et Me Ph-2-NO.sub.2 Gb Et Me Ph-2-Me Gb Et Me PhCH.sub.2 Ga Et Et Et Ga Et Pr-n Pr-n Gb Et (CH.sub.2).sub.4 Ga Et (CH.sub.2).sub.5 Ga Pr-n H Me Gc Pr-n H Et Gc Pr-n Me Me Ga Pr-n Me Et Ga Pr-n Me Ph Ga Pr-n Me PhCH.sub.2 Ga Pr-n Et Et Ga Pr-n Pr-n Pr-n Gb Pr-n (CH.sub.2).sub.4 Ga Pr-n (CH.sub.2).sub.5 Ga CH.sub.2CHCH.sub.2 H Me Gc CH.sub.2CHCH.sub.2 H Et Gc CH.sub.2CHCH.sub.2 Me Me Ga CH.sub.2CHCH.sub.2 Me Et Ga CH.sub.2CHCH.sub.2 Me Pr-n Gb CH.sub.2CHCH.sub.2 Me Pr-i Gb CH.sub.2CHCH.sub.2 Me Bu-n Gb CH.sub.2CHCH.sub.2 Me Ph Ga CH.sub.2CHCH.sub.2 Me Ph-2-Cl Gb CH.sub.2CHCH.sub.2 Me Ph-2-CO.sub.2 Me Gb CH.sub.2CHCH.sub.2 Me Ph-2-OMe Gb CH.sub.2CHCH.sub.2 Me Ph-2-CF.sub.3 Gb CH.sub.2CHCH.sub.2 Me Ph-2-NO.sub.2 Gb CH.sub.2CHCH.sub.2 Me Ph-2-Me Gb CH.sub. 2CHCH.sub.2 Me PhCH.sub.2 Ga CH.sub.2CHCH.sub.2 Et Et Ga CH.sub.2CHCH.sub.2 Pr-n pr-n Gb CH.sub.2CHCH.sub.2 (CH.sub.2).sub.4 Ga CH.sub.2CHCH.sub.2 (CH.sub.2).sub.5 Ga Ph Me Me Ga Ph Me Et Ga Ph (CH.sub.2).sub.4 Ga Ph (CH.sub.2).sub.5 Ga CHCCH.sub.2 Me Me Ga MeOCH.sub.2 Me Me Ga MeSCH.sub.2 Me Me Ga MeO.sub.2 CCH.sub.2 Me Me Ga Pr-i Me Me Gb PhCH.sub.2 Me Me Gc ______________________________________

TABLE 3 ______________________________________ ##STR146## R.sup.11 R.sup.12 R.sup.13 Gn ______________________________________ H Me Me Ga Me Me Me Ga Et Me Me Ga Pr-n Me Me Gb Pr-i Me Me Gb cyc-Pr Me Me Gb cyc-PrCH.sub.2 Me Me Gb Bu-n Me Me Gb Bu-sec Me Me Gb Bu-t Me Me Gb CH.sub.2CHCH.sub.2 Me Me Ga CHCCH.sub.2 Me Me Ga MeOCH.sub.2 Me Me Ga EtOCH.sub.2 Me Me Gb MeOCH.sub.2 CH.sub.2 Me Me Ga EtOCH.sub.2 CH.sub.2 Me Me Gb MeOCH.sub.2 (CH.sub.3)CH Me Me Gb EtOCH.sub.2 (CH.sub.3)CH Me Me Gb CHF.sub.2 OCH.sub.2 Me Me Ga MeSCH.sub.2 Me Me Ga EtSCH.sub.2 Me Me Gb MeSCH.sub.2 CH.sub.2 Me Me Ga EtSCH.sub.2 CH.sub.2 Me Me Gb MeSO.sub.2 CH.sub.2 Me Me Ga EtSO.sub.2 CH.sub.2 Me Me Gb MeSO.sub.2 CH.sub.2 CH.sub.2 Me Me Ga EtSO.sub.2 CH.sub.2 CH.sub.2 Me Me Gb FCH.sub.2 Me Me Ga ClCH.sub.2 Me Me Ga BrCH.sub.2 Me Me Ga ICH.sub.2 Me Me Ga FCH.sub.2 CH.sub.2 Me Me Ga ClCH.sub.2 CH.sub.2 Me Me Ga BrCH.sub.2 CH.sub.2 Me Me Ga ICH.sub.2 CH.sub.2 Me Me Ga FCH.sub.2 (CH.sub.3)CH Me Me Gb ClCH.sub.2 (CH.sub.3)CH Me Me Gb BrCH.sub.2 (CH.sub.3)CH Me Me Gb ICH.sub.2 (CH.sub.3)CH Me Me Gb CF.sub.3 CH.sub.2 Me Me Ga NCCH.sub.2 Me Me Ga NCCH.sub.2 CH.sub.2 Me Me Ga MeO.sub.2 CCH.sub.2 Me Me Ga EtO.sub.2 CCH.sub.2 Me Me Gb Pr-nO.sub.2 CCH.sub.2 Me Me Gc MeO.sub.2 CCH.sub.2 CH.sub.2 Me Me Ga EtO.sub.2 CCH.sub.2 CH.sub.2 Me Me Gb Pr-nO.sub.2 CCH.sub.2 CH.sub.2 Me Me Gc MeCOCH.sub.2 Me Me Ga PhCH.sub.2 Me Me Ga Ph Me Me Ga H Me Et Ga Me Me Et Ga Et Me Et Ga Pr-n Me Et Gb Pr-i Me Et Gb cyc-Pr Me Et Gb cyc-Pr CH.sub.2 Me Et Gb Bu-n Me Et Gb Bu-sec Me Et Ga Bu-t Me Et Ga CH.sub.2CHCH.sub.2 Me Et Ga CHCCH.sub.2 Me Et Gb MeOCH.sub.2 Me Et Ga EtOCH.sub.2 Me Et Ga MeOCH.sub.2 CH.sub.2 Me Et Gb EtOCH.sub.2 CH.sub.2 Me Et Gb MeOCH.sub.2 (CH.sub.3)CH Me Et Gb EtOCH.sub.2 (CH.sub.3)CH Me Et Gb CHF.sub.2 OCH.sub.2 Me Et Gb MeSCH.sub.2 Me Et Ga EtSCH.sub.2 Me Et Ga MeSCH.sub.2 CH.sub.2 Me Et Gb EtSCH.sub.2 CH.sub.2 Me Et Ga MeSO.sub.2 CH.sub.2 Me Et Gb EtSO.sub.2 CH.sub.2 Me Et Ga MeSO.sub.2 CH.sub.2 CH.sub.2 Me Et Gb EtSO.sub.2 CH.sub.2 CH.sub.2 Me Et Gb FCH.sub.2 Me Et Ga ClCH.sub.2 Me Et Ga BrCH.sub.2 Me Et Ga ICH.sub.2 Me Et Ga FCH.sub.2 CH.sub.2 Me Et Ga ClCH.sub.2 CH.sub.2 Me Et Ga BrCH.sub.2 CH.sub.2 Me Et Ga ICH.sub.2 CH.sub.2 Me Et Ga FCH.sub.2 (CH.sub.3)CH Me Et Gb ClCH.sub.2 (CH.sub.3)CH Me Et Gb BrCH.sub.2 (CH.sub.3)CH Me Et Gb ICH.sub.2 (CH.sub.3)CH Me Et Gb CF.sub.3 CH.sub.2 Me Et Ga NCCH.sub.2 Me Et Ga NCCH.sub.2 CH.sub.2 Me Et Ga MeO.sub.2 CCH.sub.2 Me Et Ga EtO.sub.2 CCH.sub.2 Me Et Gb Pr-nO.sub.2 CCH.sub.2 Me Et Gc MeO.sub.2 CCH.sub.2 CH.sub.2 Me Et Ga EtO.sub.2 CCH.sub.2 CH.sub.2 Me Et Gb Pr-nO.sub.2 CCH.sub.2 CH.sub.2 Me Et Gc MeCOCH.sub.2 Me Et Ga PhCH.sub.2 Me Et Ga Ph Me Et Ga H Me Pr-n Ga Me Me Pr-n Ga Et Me Pr-n Ga Pr-n Me Pr-n Gb Pr-i Me Pr-n Gb cyc-Pr Me Pr-n Gb CH.sub.2CHCH.sub.2 Me Pr-n Ga CHCCH.sub.2 Me Pr-n Ga MeOCH.sub.2 Me Pr-n Ga MeOCH.sub.2 CH.sub.2 Me Pr-n Ga CHF.sub.2 OCH.sub.2 Me Pr-n Ga MeSCH.sub.2 Me Pr-n Ga MeSCH.sub.2 CH.sub.2 Me Pr-n Ga MeSO.sub.2 CH.sub.2 Me Pr-n Ga MeSO.sub.2 CH.sub.2 CH.sub.2 Me Pr-n Ga FCH.sub.2 Me Pr-n Ga ClCH.sub.2 Me Pr-n Ga BrCH.sub.2 Me Pr-n Ga ICH.sub.2 Me Pr-n Ga FCH.sub.2 CH.sub.2 Me Pr-n Ga ClCH.sub.2 CH.sub.2 Me Pr-n Ga BrCH.sub.2 CH.sub.2 Me Pr-n Ga ICH.sub.2 CH.sub.2 Me Pr-n Ga CF.sub.3 CH.sub.2 Me Pr-n Ga NCCH.sub.2 Me Pr-n Ga NCCH.sub.2 CH.sub.2 Me Pr-n Ga MeO.sub.2 CCH.sub.2 Me Pr-n Ga MeCOCH.sub.2 Me Pr-n Ga PhCH.sub.2 Me Pr-n Ga Ph Me Pr-n Ga H Et Me Ga Me Et Me Ga Et Et Me Ga Pr-n Et Me Gb Pr-i Et Me Gb cyc-Pr Et Me Gb cyc-PrCH.sub.2 Et Me Gb Bu-n Et Me Gb Bu-sec Et Me Gb Bu-t Et Me Gb CH.sub.2CHCH.sub.2 Et Me Ga CHCCH.sub.2 Et Me Ga MeOCH.sub.2 Et Me Ga EtOCH.sub.2 Et Me Gb MeOCH.sub.2 CH.sub.2 Et Me Ga EtOCH.sub.2 CH.sub.2 Et Me Gb MeOCH.sub.2 (CH.sub.3)CH Et Me Gb EtOCH.sub.2 (CH.sub.3)CH Et Me Gb CHF.sub.2 OCH.sub.2 Et Me Ga MeSCH.sub.2 Et Me Ga EtSCH.sub.2 Et Me Gb MeSCH.sub.2 CH.sub.2 Et Me Ga EtSCH.sub.2 CH.sub.2 Et Me Gb MeSO.sub.2 CH.sub.2 Et Me Ga EtSO.sub.2 CH.sub.2 Et Me Gb MeSO.sub.2 CH.sub.2 CH.sub.2 Et Me Gb EtSO.sub.2 CH.sub.2 CH.sub.2 Et Me Ga FCH.sub.2 Et Me Ga ClCH.sub.2 Et Me Ga BrCH.sub.2 Et Me Ga ICH.sub.2 Et Me Ga FCH.sub.2 CH.sub.2 Et Me Ga ClCH.sub.2 CH.sub.2 Et Me Ga BrCH.sub.2 CH.sub.2 Et Me Ga ICH.sub.2 CH.sub.2

Et Me Ga FCH.sub.2 (CH.sub.3)CH Et Me Gb ClCH.sub.2 (CH.sub.3)CH Et Me Gb BrCH.sub.2 (CH.sub.3)CH Et Me Gb ICH.sub.2 (CH.sub.3)CH Et Me Gb CF.sub.3 CH.sub.2 Et Me Ga NCCH.sub.2 Et Me Ga NCCH.sub.2 CH.sub.2 Et Me Ga MeO.sub.2 CCH.sub.2 Et Me Ga EtO.sub.2 CCH.sub.2 Et Me Gb Pr-nO.sub.2 CCH.sub.2 Et Me Gc MeO.sub.2 CCH.sub.2 CH.sub.2 Et Me Ga EtO.sub.2 CCH.sub.2 CH.sub.2 Et Me Gb Pr-nO.sub.2 CCH.sub.2 CH.sub.2 Et Me Gc MeCOCH.sub.2 Et Me Ga PhCH.sub.2 Et Me Ga Ph Et Me Ga H Pr-n Me Ga Me Pr-n Me Ga Et Pr-n Me Ga Pr-n Pr-n Me Gb Pr-i Pr-n Me Gb cyc-Pr Pr-n Me Gb CH.sub.2CHCH.sub.2 Pr-n Me Ga CHCCH.sub.2 Pr-n Me Ga MeOCH.sub.2 Pr-n Me Ga MeSCH.sub.2 Pr-n Me Ga MeSCH.sub.2 CH.sub.2 Pr-n Me Ga MeSO.sub.2 CH.sub.2 Pr-n Me Ga MeSO.sub.2 CH.sub.2 CH.sub.2 Pr-n Me Ga FCH.sub.2 Pr-n Me Ga ClCH.sub.2 Pr-n Me Ga BrCH.sub.2 Pr-n Me Ga ICH.sub.2 Pr-n Me Ga FCH.sub.2 CH.sub.2 Pr-n Me Ga ClCH.sub.2 CH.sub.2 Pr-n Me Ga BrCH.sub.2 CH.sub.2 Pr-n Me Ga ICH.sub.2 CH.sub.2 Pr-n Me Ga CF.sub.3 CH.sub.2 Pr-n Me Ga NCCH.sub.2 Pr-n Me Ga NCCH.sub.2 CH.sub.2 Pr-n Me Ga MeO.sub.2 CCH.sub.2 Pr-n Me Ga MeCOCH.sub.2 Pr-n Me Ga PhCH.sub.2 Pr-n Me Ga Ph Pr-n Me Ga H Et Et Ga Me Et Et Ga Et Et Et Ga Pr-n Et Et Gb Pr-i Et Et Gb cyc-Pr Et Et Gb CH.sub.2CHCH.sub.2 Et Et Ga CHCCH.sub.2 Et Et Ga MeOCH.sub.2 Et Et Ga MeOCH.sub.2 CH.sub.2 Et Et Ga MeSCH.sub.2 Et Et Ga MeSCH.sub.2 CH.sub.2 Et Et Ga MeSO.sub.2 CH.sub.2 Et Et Ga MeSO.sub.2 CH.sub.2 CH.sub.2 Et Et Ga FCH.sub.2 Et Et Ga ClCH.sub.2 Et Et Ga BrCH.sub.2 Et Et Ga ICH.sub.2 Et Et Ga FCH.sub.2 CH.sub.2 Et Et Ga ClCH.sub.2 CH.sub.2 Et Et Ga BrCH.sub.2 CH.sub.2 Et Et Ga ICH.sub.2 CH.sub.2 Et Et Ga CF.sub.3 CH.sub.2 Et Et Ga NCCH.sub.2 Et Et Ga NCCH.sub.2 CH.sub.2 Et Et Ga MeO.sub.2 CCH.sub.2 Et Et Ga MeO.sub.2 CCH.sub.2 CH.sub.2 Et Et Ga MeCOCH.sub.2 Et Et Ga PhCH.sub.2 Et Et Ga Ph Et Et Ga H CH.sub.2CHCH.sub.2 Me Ga Me CH.sub.2CHCH.sub.2 Me Ga Et CH.sub.2CHCH.sub.2 Me Ga Pr-n CH.sub.2CHCH.sub.2 Me Gb Pr-i CH.sub.2CHCH.sub.2 Me Gb cyc-Pr CH.sub.2 CHCH.sub.2 Me Gb cyc-PrCH.sub.2 CH.sub.2CHCH.sub.2 Me Gb Bu-n CH.sub.2CHCH.sub.2 Me Gb Bu-sec CH.sub.2CHCH.sub.2 Me Gb Bu-t CH.sub.2CHCH.sub.2 Me Gb CH.sub.2CHCH.sub.2 CH.sub.2CHCH.sub.2 Me Ga CHCCH.sub.2 CH.sub.2CHCH.sub.2 Me Ga MeOCH.sub.2 CH.sub.2CHCH.sub.2 Me Ga EtOCH.sub.2 CH.sub.2CHCH.sub.2 Me Gb MeOCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Ga EtOCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Gb MeOCH.sub.2 (CH.sub.3)CH CH.sub.2CHCH.sub.2 Me Gb EtOCH.sub.2 (CH.sub.3)CH CH.sub.2CHCH.sub.2 Me Gb CHF.sub.2 OCH.sub.2 CH.sub.2CHCH.sub.2 Me Ga MeSCH.sub.2 CH.sub.2CHCH.sub.2 Me Ga EtSCH.sub.2 CH.sub.2CHCH.sub.2 Me Gb MeSCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Ga EtSCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Gb MeSO.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Ga EtSO.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Gb MeSO.sub.2 CH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Ga EtSO.sub.2 CH.sub. 2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Gb FCH.sub.2 CH.sub.2CHCH.sub.2 Me Ga ClCH.sub.2 CH.sub.2CHCH.sub.2 Me Ga BrCH.sub.2 CH.sub.2CHCH.sub.2 Me Ga ICH.sub.2 CH.sub.2CHCH.sub.2 Me Ga FCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Ga ClCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Ga BrCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Ga ICH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Ga FCH.sub.2 (CH.sub.3)CH CH.sub.2CHCH.sub.2 Me Gb ClCH.sub.2 (CH.sub.3)CH CH.sub.2CHCH.sub.2 Me Gb BrCH.sub.2 (CH.sub.3)CH CH.sub.2CHCH.sub.2 Me Gb ICH.sub.2 (CH.sub.3)CH CH.sub.2CHCH.sub.2 Me Gb CF.sub.3 CH.sub.2 CH.sub.2CHCH.sub.2 Me Ga NCCH.sub.2 CH.sub.2CHCH.sub.2 Me Ga NCCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Ga MeO.sub.2 CCH.sub.2 CH.sub.2CHCH.sub.2 Me Ga EtO.sub.2 CCH.sub.2 CH.sub.2CHCH.sub.2 Me Gb Pr-nO.sub.2 CCH.sub.2 CH.sub.2CHCH.sub.2 Me Gc MeO.sub.2 CCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Ga EtO.sub.2 CCH.sub.2 CH.sub. 2 CH.sub.2CHCH.sub.2 Me Gb Pr-nO.sub.2 CCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Me Gc MeCOCH.sub.2 CH.sub.2CHCH.sub.2 Me Ga PhCH.sub.2 CH.sub.2CHCH.sub.2 Me Ga Ph CH.sub.2CHCH.sub.2 Me Ga H CH.sub.2CHCH.sub.2 Et Ga Me CH.sub.2CHCH.sub.2 Et Ga Et CH.sub.2CHCH.sub.2 Et Ga Pr-n CH.sub.2CHCH.sub.2 Et Gb Pr-i CH.sub.2CHCH.sub.2 Et Gb cyc-Pr CH.sub.2CHCH.sub.2 Et Gb

cyc-PrCH.sub.2 CH.sub.2CHCH.sub.2 Et Gb Bu-n CH.sub.2CHCH.sub.2 Et Gb Bu-sec CH.sub.2CHCH.sub.2 Et Gb Bu-t CH.sub.2CHCH.sub.2 Et Gb CH.sub.2CHCH.sub.2 CH.sub.2CHCH.sub.2 Et Ga CHCCH.sub.2 CH.sub.2CHCH.sub.2 Et Ga MeOCH.sub.2 CH.sub.2CHCH.sub.2 Et Ga EtOCH.sub.2 CH.sub.2CHCH.sub.2 Et Gb MeOCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Ga EtOCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Gb MeOCH.sub.2 (CH.sub.3)CH CH.sub.2CHCH.sub.2 Et Gb EtOCH.sub.2 (CH.sub.3)CH CH.sub.2CHCH.sub.2 Et Gb CHF.sub.2 OCH.sub.2 CH.sub.2CHCH.sub.2 Et Ga MeSCH.sub.2 CH.sub.2CHCH.sub.2 Et Ga EtSCH.sub.2 CH.sub.2CHCH.sub.2 Et Gb MeSCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Ga EtSCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Gb MeSO.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Ga EtSO.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Gb MeSO.sub.2 CH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Ga EtSO.sub.2 CH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Gb FCH.sub.2 CH.sub.2CHCH.sub.2 Et Ga ClCH.sub.2 CH.sub.2CHCH.sub.2 Et Ga BrCH.sub.2 CH.sub.2CHCH.sub.2 Et Ga ICH.sub.2 CH.sub.2CHCH.sub.2 Et Ga FCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Ga ClCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Ga BrCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Ga ICH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Ga FCH.sub.2 (CH.sub.3)CH CH.sub.2CHCH.sub.2 Et Gb ClCH.sub.2 (CH.sub.3)CH CH.sub.2CHCH.sub.2 Et Gb BrCH.sub.2 (CH.sub.3)CH CH.sub.2CHCH.sub.2 Et Gb ICH.sub.2 (CH.sub.3)CH CH.sub.2CHCH.sub.2 Et Gb CF.sub.3 CH.sub.2 CH.sub.2CHCH.sub.2 Et Ga NCCH.sub.2 CH.sub.2CHCH.sub.2 Et Ga NCCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Ga MeO.sub.2 CCH.sub.2 CH.sub.2CHCH.sub.2 Et Ga EtO.sub.2 CCH.sub.2 CH.sub.2CHCH.sub.2 Et Gb Pr-nO.sub.2 CCH.sub.2 CH.sub.2CHCH.sub.2 Et Gc MeO.sub.2 CCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Ga EtO.sub.2 CCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Gb Pr-nO.sub.2 CCH.sub.2 CH.sub.2 CH.sub.2CHCH.sub.2 Et Gc MeCOCH.sub.2 CH.sub.2CHCH.sub.2 Et Ga PhCH.sub.2 CH.sub.2CHCH.sub.2 Et Ga Ph CH.sub.2CHCH.sub.2 Et Ga H Ph Me Ga Me Ph Me Ga Et Ph Me Ga Pr-n Ph Me Gb Pr-i Ph Me Gb cyc-Pr Ph Me Gb cyc-PrCH.sub.2 Ph Me Gb Bu-n Ph Me Gb Bu-sec Ph Me Gb Bu-t Ph Me Gb CH.sub.2CHCH.sub.2 Ph Me Ga CHCCH.sub.2 Ph Me Ga MeOCH.sub.2 Ph Me Ga EtOCH.sub.2 Ph Me Gb MeOCH.sub.2 CH.sub. 2 Ph Me Ga EtOCH.sub.2 CH.sub.2 Ph Me Gb MeOCH.sub.2 (CH.sub.3)CH Ph Me Gb EtOCH.sub.2 (CH.sub.3)CH Ph Me Gb CHF.sub.2 OCH.sub.2 Ph Me Ga MeSCH.sub.2 Ph Me Ga EtSCH.sub.2 Ph Me Gb MeSCH.sub.2 CH.sub.2 Ph Me Ga EtSCH.sub.2 CH.sub.2 Ph Me Gb MeSO.sub.2 CH.sub.2 Ph Me Ga EtSO.sub.2 CH.sub.2 Ph Me Gb MeSO.sub.2 CH.sub.2 CH.sub.2 Ph Me Gb EtSO.sub.2 CH.sub.2 CH.sub.2 Ph Me Ga FCH.sub.2 Ph Me Ga ClCH.sub.2 Ph Me Ga BrCH.sub.2 Ph Me Ga ICH.sub.2 Ph Me Ga FCH.sub.2 CH.sub.2 Ph Me Ga ClCH.sub.2 CH.sub.2 Ph Me Ga BrCH.sub.2 CH.sub.2 Ph Me Ga ICH.sub.2 CH.sub.2 Ph Me Ga FCH.sub.2 (CH.sub.3)CH Ph Me Gb ClCH.sub.2 (CH.sub.3)CH Ph Me Gb BrCH.sub.2 (CH.sub.3)CH Ph Me Gb ICH.sub.2 (CH.sub.3)CH Ph Me Gb CF.sub.3 CH.sub.2 Ph Me Ga NCCH.sub.2 Ph Me Ga NCCH.sub.2 CH.sub.2 Ph Me Ga MeO.sub.2 CCH.sub.2 Ph Me Ga EtO.sub.2 CCH.sub.2 Ph Me Gb Pr-nO.sub.2 CCH.sub.2 Ph Me Gc MeO.sub.2 CCH.sub.2 CH.sub.2 Ph Me Ga EtO.sub.2 CCH.sub.2 CH.sub.2 Ph Me Gb Pr-nO.sub.2 CCH.sub.2 CH.sub.2 Ph Me Gc MeCOCH.sub.2 Ph Me Ga PhCH.sub.2 Ph Me Ga Ph Ph Me Ga H Ph Et Ga Me Ph Et Ga Et Ph Et Ga Pr-n Ph Et Gb Pr-i Ph Et Gb cyc-Pr Ph Et Gb cyc-PrCH.sub.2 Ph Et Gb Bu-n Ph Et Gb Bu-sec Ph Et Gb Bu-t Ph Et Gb CH.sub.2CHCH.sub.2 Ph Et Ga CHCCH.sub.2 Ph Et Ga MeOCH.sub.2 Ph Et Ga EtOCH.sub.2 Ph Et Gb MeOCH.sub.2 CH.sub.2 Ph Et Ga EtOCH.sub.2 CH.sub.2 Ph Et Gb MeOCH.sub.2 (CH.sub.3)CH Ph Et Gb EtOCH.sub.2 (CH.sub.3)CH Ph Et Gb CHF.sub.2 OCH.sub.2 Ph Et Ga MeSCH.sub.2 Ph Et Ga EtSCH.sub.2 Ph Et Gb MeSCH.sub.2 CH.sub.2 Ph Et Ga EtSCH.sub.2 CH.sub.2 Ph Et Gb MeSO.sub.2 CH.sub.2 Ph Et Ga EtSO.sub.2 CH.sub.2 Ph Et Gb MeSO.sub.2 CH.sub.2 CH.sub.2 Ph Et Ga EtSO.sub.2 CH.sub.2 CH.sub.2 Ph Et Gb FCH.sub.2 Ph Et Ga ClCH.sub.2 Ph Et Ga BrCH.sub.2 Ph Et Ga ICH.sub.2 Ph Et Ga FCH.sub.2 CH.sub.2 Ph Et Ga ClCH.sub.2 CH.sub.2 Ph Et Ga BrCH.sub.2 CH.sub.2 Ph Et Ga ICH.sub.2 CH.sub.2 Ph Et Ga FCH.sub.2 (CH.sub.3)CH Ph Et Gb ClCH.sub.2 (CH.sub.3)CH Ph Et Gb BrCH.sub.2 (CH.sub.3)CH Ph Et Gb

ICH.sub.2 (CH.sub.3)CH Ph Et Gb CF.sub.3 CF.sub.2 Ph Et Ga NCCH.sub.2 Ph Et Ga NCCH.sub.2 CH.sub.2 Ph Et Ga MeO.sub.2 CCH.sub.2 Ph Et Ga EtO.sub.2 CCH.sub.2 Ph Et Gb Pr-nO.sub.2 CCH.sub.2 Ph Et Gc MeO.sub.2 CCH.sub.2 CH.sub.2 Ph Et Ga EtO.sub.2 CCH.sub.2 CH.sub.2 Ph Et Gb Pr-nO.sub.2 CCH.sub.2 CH.sub.2 Ph Et Gc MeCOCH.sub.2 Ph Et Ga PhCH.sub.2 Ph Et Ga Ph Ph Et Ga H (CH.sub.2).sub.3 Ga Me (CH.sub.2).sub.3 Ga Et (CH.sub.2).sub.3 Ga Pr-n (CH.sub.2).sub.3 Gb Pr-i (CH.sub.2).sub.3 Gb cyc-Pr (CH.sub.2).sub.3 Gb cyc-PrCH.sub.2 (CH.sub.2).sub.3 Gb Bu-n (CH.sub.2).sub.3 Gb Bu-sec (CH.sub.2).sub.3 Gb Bu-t (CH.sub.2).sub.3 Gb CH.sub.2CHCH.sub.2 (CH.sub.2).sub.3 Ga CHCCH.sub.2 (CH.sub.2).sub.3 Ga MeOCH.sub.2 (CH.sub.2).sub.3 Ga EtOCH.sub.2 (CH.sub.2).sub.3 Gb MeOCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Ga EtOCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Gb MeOCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.3 Gb EtOCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.3 Gb CHF.sub.2 OCH.sub.2 (CH.sub.2).sub.3 Ga MeSCH.sub.2 (CH.sub.2).sub.3 Ga EtSCH.sub.2 (CH.sub.2).sub.3 Gb MeSCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Ga EtSCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Gb MeSO.sub.2 CH.sub.2 (CH.sub.2).sub.3 Ga

EtSO.sub.2 CH.sub.2 (CH.sub.2).sub.3 Gb MeSO.sub.2 CH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Gb EtSO.sub.2 CH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Ga FCH.sub.2 (CH.sub.2).sub.3 Ga ClCH.sub.2 (CH.sub.2).sub.3 Ga BrCH.sub.2 (CH.sub.2).sub.3 Ga ICH.sub.2 (CH.sub.2).sub.3 Ga FCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Ga ClCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Ga BrCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Ga ICH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Ga FCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.3 Gb ClCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.3 Gb BrCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.3 Gb ICH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.3 Gb CF.sub.3 CH.sub.2 (CH.sub.2).sub.3 Ga NCCH.sub.2 (CH.sub. 2).sub.3 Ga NCCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Ga MeO.sub.2 CCH.sub.2 (CH.sub.2).sub.3 Ga EtO.sub.2 CCH.sub.2 (CH.sub.2).sub.3 Gb Pr-nO.sub.2 CCH.sub.2 (CH.sub.2).sub.3 Gc MeO.sub.2 CCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Ga EtO.sub.2 CCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Gb Pr-nO.sub.2 CCH.sub.2 CH.sub.2 (CH.sub.2).sub.3 Gc MeCOCH.sub.2 (CH.sub.2).sub.3 Ga PhCH.sub.2 (CH.sub.2).sub.3 Ga Ph (CH.sub.2).sub.3 Ga H (CH.sub.2).sub.4 Ga Me (CH.sub.2).sub.4 Ga Et (CH.sub.2).sub.4 Ga Pr-n (CH.sub.2).sub.4 Gb Pr-i (CH.sub.2).sub.4 Gb cyc-Pr (CH.sub.2).sub.4 Gb cyc-PrCH.sub.2 (CH.sub.2).sub.4 Gb Bu-n (CH.sub.2).sub.4 Gb Bu-sec (CH.sub.2).sub.4 Gb Bu-t (CH.sub.2).sub.4 Gb CH.sub.2CHCH.sub.2 (CH.sub.2).sub.4 Ga CHCCH.sub.2 (CH.sub.2).sub.4 Ga MeOCH.sub.2 (CH.sub.2).sub.4 Ga EtOCH.sub.2 (CH.sub.2).sub.4 Gb MeOCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga EtOCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Gb MeOCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.4 Gb EtOCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.4 Gb CHF.sub.2 OCH.sub.2 (CH.sub.2).sub.4 Ga MeSCH.sub.2 (CH.sub.2).sub.4 Ga EtSCH.sub.2 (CH.sub.2).sub.4 Gb MeSCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga EtSCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Gb MeSO.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga EtSO.sub.2 CH.sub.2 (CH.sub.2).sub.4 Gb MeSO.sub.2 CH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga EtSO.sub.2 CH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Gb FCH.sub.2 (CH.sub.2).sub.4 Ga ClCH.sub.2 (CH.sub.2).sub.4 Ga BrCH.sub.2 (CH.sub.2).sub.4 Ga ICH.sub.2 (CH.sub.2).sub.4 Ga FCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga ClCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga BrCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga ICH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga FCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.4 Gb ClCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.4 Gb BrCH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.4 Gb ICH.sub.2 (CH.sub.3)CH (CH.sub.2).sub.4 Gb CF.sub.3 CH.sub.2 (CH.sub.2).sub.4 Ga NCCH.sub.2 (CH.sub.2).sub.4 Ga NCCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga MeO.sub.2 CCH.sub.2 (CH.sub.2).sub.4 Ga EtO.sub.2 CCH.sub.2 (CH.sub.2).sub.4 Gb Pr-nO.sub.2 CCH.sub.2 (CH.sub.2).sub.4 Gc MeO.sub.2 CCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Ga EtO.sub.2 CCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Gb Pr-nO.sub.2 CCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Gc MeCOCH.sub.2 (CH.sub.2).sub.4 Ga PhCH.sub.2 (CH.sub.2).sub.4 Ga Ph (CH.sub.2).sub.4 Ga ______________________________________

TABLE 4 ______________________________________ ##STR147## R.sup.11 R.sup.12 R.sup.13 Gn ______________________________________ Me Me Me Gb Me Me Et Gc Me Et Et Gb Me Me Ph Gc Me (CH.sub.2).sub.4 Gb Me (CH.sub.2).sub.5 Gb Et Me Me Gb Et Me Et Gc Et Et Et Gb Et Me Ph Gc Et (CH.sub.2).sub.4 Gb Et (CH.sub.2).sub.5 Gb Pr-n Me Me Gb Pr-n Me Et Gc Pr-n Et Et Gb Pr-n Me Ph Gc Pr-n (CH.sub.2).sub.4 Gb Pr-n (CH.sub.2).sub.5 Gb CH.sub.2CHCH.sub.2 Me Me Gb CH.sub.2CHCH.sub.2 Me Et Gc CH.sub.2CHCH.sub.2 Et Et Gb CH.sub.2CHCH.sub.2 Me Ph Gc CH.sub.2CHCH.sub.2 (CH.sub.2 ).sub.4 Gb CH.sub.2CHCH.sub.2 (CH.sub.2).sub.5 Gb CHCCH.sub.2 Me Me Gb CHCCH.sub.2 Me Et Gc CHCCH.sub.2 Et Et Gb CHCCH.sub.2 Me Ph Gc CHCCH.sub.2 (CH.sub.2).sub.4 Gb CHCCH.sub.2 (CH.sub.2).sub.5 Gb MeOCH.sub.2 CH.sub.2 Me Me Gb MeOCH.sub.2 CH.sub.2 Me Et Gc MeOCH.sub.2 CH.sub.2 Et Et Gb MeOCH.sub.2 CH.sub.2 Me Ph Gc MeOCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Gb MeOCH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Gb ClCH.sub.2 CH.sub.2 Me Me Gb ClCH.sub.2 CH.sub.2 Me Et Gc ClCH.sub.2 CH.sub.2 Et Et Gb ClCH.sub.2 CH.sub.2 Me Ph Gc ClCH.sub.2 CH.sub.2 (CH.sub.2).sub.4 Gb ClCH.sub.2 CH.sub.2 (CH.sub.2).sub.5 Gb CF.sub.3 CH.sub.2 Me Me Gb CF.sub.3 CH.sub.2 Me Et Gc CF.sub.3 CH.sub.2 Et Et Gb CF.sub.3 CH.sub.2 Me Ph Gc CF.sub.3 CH.sub.2 (CH.sub.2).sub.4 Gb CF.sub.3 CH.sub.2 (CH.sub.2).sub.5 Gb NCCH.sub.2 Me Me Gb NCCH.sub.2 Me Et Gc NCCH.sub.2 Et Et Gb NCCH.sub.2 Me Ph Gc NCCH.sub.2 (CH.sub.2).sub.4 Gb NCCH.sub.2 (CH.sub.2).sub.5 Gb MeO.sub.2 CCH.sub.2 Me Me Gb MeO.sub.2 CCH.sub.2 Me Et Gc MeO.sub.2 CCH.sub.2 Et Et Gb MeO.sub.2 CCH.sub.2 Me Ph Gc MeO.sub.2 CCH.sub.2 (CH.sub.2).sub.4 Gb MeO.sub.2 CCH.sub.2 (CH.sub.2).sub.5 Gb PhCH.sub.2 Me Me Gb PhCH.sub.2 Me Et Gc PhCH.sub.2 Et Et Gb PhCH.sub.2 Me Ph Gc PhCH.sub.2 (CH.sub.2).sub.4 Gb PhCH.sub.2 (CH.sub.2).sub.5 Gb ______________________________________

TABLE 5 ______________________________________ ##STR148## R.sup.11 R.sup.12 R.sup.13 Gn ______________________________________ Me Me Me Gb Me Me Et Gc Me Et Et Gb Me Me Ph Gc Me (CH.sub.2).sub.4 Gb Me (CH.sub.2).sub.5 Gb Et Me Me Gb Et Me Et Gc Et Et Et Gb Et Me Ph Gc Et (CH.sub.2).sub.4 Gb Et (CH.sub.2).sub.5 Gb Pr-n Me Me Gb Pr-n Me Et Gc Pr-n Et Et Gb Pr-n Me Ph Gc Pr-n (CH.sub.2).sub.4 Gb Pr-n (CH.sub.2).sub.5 Gb CH.sub.2CHCH.sub.2 Me Me Gb CH.sub.2CHCH.sub.2 Me Et Gc CH.sub.2CHCH.sub.2 Et Et Gb CH.sub.2CHCH.sub.2 Me Ph Gc CH.sub.2CHCH.sub.2 (CH.sub. 2).sub.4 Gb CH.sub.2CHCH.sub.2 (CH.sub.2).sub.5 Gb ______________________________________

TABLE 6 ______________________________________ ##STR149## R.sup.11 R.sup.12 R.sup.13 Gn ______________________________________ Me Me Me Gb Et Me Me Gb cyc-Pr Me Me Gb CH.sub.2CHCH.sub.2 Me Me Gc CHCCH.sub.2 Me Me Gc MeOCH.sub.2 Me Me Gc MeOCH.sub.2 CH.sub.2 Me Me Gc MeSCH.sub.2 Me Me Gc MeSO.sub.2 CH.sub.2 Me Me Gc ClCH.sub.2 CH.sub.2 Me Me Gc CF.sub.3 CH.sub.2 Me Me Gc NCCH.sub.2 CH.sub.2 Me Me Gc MeO.sub.2 CCH.sub.2 Me Me Gc MeCOCH.sub.2 Me Me Gc PhCH.sub.2 Me Me Gc Ph Me Me Gc Me Me Et Gb Me Me Pr-n Gb Me Et Me Gb Me Pr-n Me Gb Me Et Et Gb Me CH.sub.2CHCH.sub.2 Me Gb Me CH.sub.2CHCH.sub.2 Et Gb Me Ph Me Gb Me Ph Et Gb Me (CH.sub.2).sub.3 Gb Me (CH.sub.2).sub.4 Gb ______________________________________

TABLE 7 ______________________________________ ##STR150## R.sup.21 R.sup.22 R.sup.23 R.sup.24 Gn ______________________________________ H H H H Ga H H H Me Ga H H H Et Gb H Me H H Ga H Et H H Gb H Me H Me Gb H Me H Et Gb H H Me Me Ga H H Me Et Gb H H H CF.sub.3 Ga H H H CH.sub.2 F Ga H H H CH.sub.2 Cl Ga H H H CH.sub.2 Br Gb H H H CH.sub.2 I Gb H H H CH.sub.2 OMe Ga H H H CH.sub.2 OEt Ga H H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga H H H CH.sub.2 OCH.sub.2 CCH Ga H H H CH.sub.2 OCHF.sub. 2 Ga H H H CH.sub.2 OCF.sub.3 Ga H H H CH.sub.2 SMe Ga H H H CH.sub.2 SEt Ga H H H CH.sub.2 SO.sub.2 Me Ga H H H CH.sub.2 SO.sub.2 Et Ga H H H CH.sub.2 CF.sub.3 Ga H H H CH.sub.2 CN Ga H H H CO.sub.2 Me Ga H H H CO.sub.2 Et Ga H H H CH.sub.2 CO.sub.2 Me Ga H H H CH.sub.2 CO.sub.2 Et Ga H H H COMe Ga H H H COEt Ga H H H CH.sub.2 COMe Ga H H H CH.sub.2 COEt Ga Me H H H Ga Me H H Me Ga Me H H Et Gb Me H H Pr-n Gb Me H H Pr-i Gb Me H H Bu-n Gc Me Me H H Ga Me Et H H Gb Me Me H Me Gb Me Me H Et Gb Me H Me Me Ga Me H Me Et Gb Me H H F Ga Me H H Cl Ga Me H H Br Gb Me H H I Gb Me H H CF.sub.3 Ga Me H H CH.sub.2 F Ga Me H H CH.sub.2 Cl Ga Me H H CH.sub.2 Br Gb Me H H CH.sub.2 I Gb Me H H CH.sub.2 CH.sub.2 F Ga Me H H CH.sub.2 CH.sub.2 Cl Ga Me H H CH.sub.2 CH.sub.2 Br Gb Me H H CH.sub.2 CH.sub.2 I Gb Me H H CH(CH.sub.3)CH.sub.2 F Ga Me H H CH(CH.sub.3)CH.sub.2 Cl Ga Me H H CH(CH.sub.3)CH.sub.2 Br Gb Me H H CH(CH.sub.3 CH.sub.2 I Gb Me H H CH.sub.2 OMe Ga Me H H CH.sub.2 OEt Ga Me H H CH.sub.2 CH.sub.2 OMe Ga Me H H CH.sub.2 CH.sub.2 OEt Ga Me H H CH(CH.sub.3)CH.sub.2 OMe Gb Me H H CH(CH.sub.3)CH.sub.2 OEt Gb Me H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga Me H H CH.sub.2 OCH.sub.2 CCH Ga Me H H CH.sub.2 OCHF.sub.2 Ga Me H H CH.sub.2 OCF.sub.3 Ga Me H H CH.sub. 2 SMe Ga Me H H CH.sub.2 SEt Ga Me H H CH.sub.2 SO.sub.2 Me Ga Me H H CH.sub.2 SO.sub.2 Et Ga Me H H CH.sub.2 CF.sub.3 Ga Me H H CH.sub.2 CN Ga Me H H CO.sub.2 Me Ga Me H H CO.sub.2 Et Ga Me H H CO.sub.2 Pr-n Gb Me H H CH.sub.2 CO.sub.2 Me Ga Me H H CH.sub.2 CO.sub.2 Et Ga Me H H CH.sub.2 CO.sub.2 Pr-n Gb Me H H COMe Ga Me H H COEt Ga Me H H COPr-n Gb Me H H CH.sub.2 COMe Ga Me H H CH.sub.2 COEt Ga Et H H H Ga Et H H Me Ga Et H H Et Gb Et H H Pr-n Gb Et H H Pr-i Gb Et H H Bu-n Gc Et Me H H Ga Et Et H H Gb Et Me H Me Gb Et Me H Et Gb Et H Me Me Ga Et H Me Et Gb Et H H F Ga Et H H Cl Ga Et H H Br Gb Et H H I Gb Et H H CF.sub.3 Ga Et H H CH.sub.2 F Ga Et H H CH.sub.2 Cl Ga Et H H CH.sub.2 Br Gb Et H H CH.sub.2 I Gb Et H H CH.sub.2 CH.sub.2 F Ga Et H H CH.sub.2 CH.sub.2 Cl Ga Et H H CH.sub.2 CH.sub.2 Br Gb Et H H CH.sub.2 CH.sub.2 I Gb Et H H CH(CH.sub.3)CH.sub.2 F Ga Et H H CH(CH.sub.3)CH.sub.2 Cl Ga Et H H CH(CH.sub.3)CH.sub.2 Br Gb Et H H CH(CH.sub.3)CH.sub.2 I Gb Et H H CH.sub.2 OMe Ga Et H H CH.sub.2 OEt Ga Et H H CH.sub.2 CH.sub.2 OMe Ga Et H H CH.sub.2 CH.sub.2 OEt Ga Et H H CH(CH.sub.3)CH.sub.2 OMe Gb Et H H CH(CH.sub.3)CH.sub.2 OEt Gb Et H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga Et H H CH.sub.2 OCH.sub.2 CCH Ga Et H H CH.sub.2 OCHF.sub.2 Ga Et H H CH.sub.2 OCF.sub.3 Ga Et H H CH.sub.2 SMe Ga Et H H CH.sub.2 SEt Ga Et H H CH.sub.2 SO.sub.2 Me Ga Et H H CH.sub.2 SO.sub.2 Et Ga Et H H CH.sub.2 CF.sub.3 Ga Et H H CH.sub.2 CN Ga Et H H CO.sub.2 Me Ga Et H H CO.sub.2 Et Ga Et H H CO.sub.2 Pr-n Gb Et H H CH.sub.2 CO.sub.2 Me Ga Et H H CH.sub.2 CO.sub.2 Et Ga Et H H CH.sub.2 CO.sub.2 Pr-n Gb Et H H COMe Ga Et H H COEt Ga Et H H COPr-n Gb Et H H CH.sub.2 COMe Ga Et H H CH.sub.2 COEt Ga Pr-n H H H Ga Pr-n H H Me Ga Pr-n H H Et Gb Pr-n Me H H Ga Pr-n Et H H Gb Pr-n Me H Me Gb Pr-n Me H Et Gb Pr-n H Me Me Ga Pr-n H Me Et Gb Pr-n H H CF.sub.3 Ga Pr-n H H CH.sub.2 F Ga Pr-n H H CH.sub.2 Cl Ga Pr-n H H CH.sub.2 Br Gb Pr-n H H CH.sub.2 I Gb Pr-n H H CH.sub.2 OMe Ga Pr-n H H CH.sub.2 OEt Ga Pr-n H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga Pr-n H H CH.sub.2 OCH.sub.2 CCH Ga Pr-n H H CH.sub.2 OCHF.sub.2 Ga Pr-n H H CH.sub.2 OCF.sub.3 Ga Pr-n H H CH.sub.2 SMe Ga Pr-n H H CH.sub.2 SEt Ga Pr-n H H CH.sub.2 SO.sub.2 Me Ga Pr-n H H CH.sub.2 SO.sub.2 Et Ga Pr-n H H CH.sub.2 CF.sub.3 Ga Pr-n H H CH.sub.2 CN Ga Pr-n H H CO.sub.2 Me Ga Pr-n H H CO.sub.2 Et Ga Pr-n H H CH.sub.2 CO.sub.2 Me Ga Pr-n H H CH.sub.2 CO.sub.2 Et Ga Pr-n H H COMe Ga Pr-n H H COEt Ga Pr-n H H CH.sub.2 COMe Ga Pr-n H H CH.sub.2 COEt Ga Pr-i H H H Ga Pr-i H H Me Ga Pr-i H H Et Gb Pr-i Me H H Ga Pr-i Et H H Gb Pr-i Me H Me Gb

Pr-i Me H Et Gb Pr-i H Me Me Ga Pr-i H Me Et Gb Pr-i H H CF.sub.3 Ga Pr-i H H CH.sub.2 F Ga Pr-i H H CH.sub.2 Cl Ga Pr-i H H CH.sub.2 Br Gb Pr-i H H CH.sub.2 I Gb Pr-i H H CH.sub.2 OMe Ga Pr-i H H CH.sub.2 OEt Ga Pr-i H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga Pr-i H H CH.sub.2 OCH.sub.2 CCH Ga Pr-i H H CH.sub.2 OCHF.sub.2 Ga Pr-i H H CH.sub.2 OCF.sub.3 Ga Pr-i H H CH.sub.2 SMe Ga Pr-i H H CH.sub.2 SEt Ga Pr-i H H CH.sub.2 SO.sub.2 Me Ga Pr-i H H CH.sub.2 SO.sub.2 Et Ga Pr-i H H CH.sub.2 CF.sub.3 Ga Pr-i H H CH.sub.2 CN Ga Pr-i H H CO.sub.2 Me Ga Pr-i H H CO.sub.2 Et Ga Pr-i H H CH.sub.2 CO.sub.2 Me Ga Pr-i H H CH.sub.2 CO.sub.2 Et Ga Pr-i H H COMe Ga Pr-i H H COEt Ga Pr-i H H CH.sub.2 COMe Ga Pr-i H H CH.sub.2 COEt Ga Bu-n H H H Ga Bu-n H H Me Ga Bu-n Me H H Ga Bu-n Me H Me Gb Bu-n H Me Me Ga Bu-n H H CF.sub.3 Ga Bu-n H H CH.sub.2 F Ga Bu-n H H CH.sub.2 Cl Ga Bu-n H H CH.sub.2 Br Gb Bu-n H H CH.sub.2 I Gb Bu-n H H CH.sub.2 OMe Ga Bu-n H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga Bu-n H H CH.sub.2 OCH.sub.2 CCH Ga Bu-n H H CH.sub.2 OCHF.sub.2 Ga Bu-n H H CH.sub.2 OCF.sub.3 Ga Bu-n H H CH.sub.2 SMe Ga Bu-n H H CH.sub.2 SO.sub.2 Me Ga Bu-n H H CH.sub.2 CF.sub.3 Ga Bu-n H H CH.sub.2 CN Ga Bu-n H H CO.sub.2 Me Ga Bu-n H H CH.sub.2 CO.sub.2 Me Ga Bu-n H H COMe Ga Bu-n H H CH.sub.2 COMe Ga CH.sub.2 CHCH.sub.2 H H H Ga CH.sub.2 CHCH.sub.2 H H Me Gb CH.sub.2 CHCH.sub.2 H H Et Gb CH.sub.2 CHCH.sub.2 Me H H Ga CH.sub.2 CHCH.sub.2 Et H H Gb CH.sub.2 CHCH.sub.2 Me H Me Gb CH.sub.2 CHCH.sub.2 Me H Et Gb CH.sub.2 CHCH.sub.2 H Me Me Ga CH.sub.2 CHCH.sub.2 H Me Et Gb CH.sub.2 CHCH.sub.2 H H CF.sub.3 Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 F Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 Cl Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 Br Gb CH.sub.2 CHCH.sub.2 H H CH.sub.2 I Gb CH.sub.2 CHCH.sub.2 H H CH.sub.2 OMe Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 OEt Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 OCHF.sub.2 Ga CH.sub. 2 CHCH.sub.2 H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 SMe Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 SEt Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 CN Ga CH.sub.2 CHCH.sub.2 H H CO.sub.2 Me Ga CH.sub.2 CHCH.sub.2 H H CO.sub.2 Et Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 CHCH.sub.2 H H COMe Ga CH.sub.2 CHCH.sub.2 H H COEt Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 COMe Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 COEt Ga CH.sub.2 CCH H H H Ga CH.sub.2 CCH H H Me Gb CH.sub.2 CCH H H Et Gb CH.sub.2 CCH Me H H Ga CH.sub.2 CCH Et H H Gb CH.sub.2 CCH Me H Me Gb CH.sub.2 CCH Me H Et Gb CH.sub.2 CCH H Me Me Ga CH.sub.2 CCH H H F Ga CH.sub.2 CCH H Me Et Gb CH.sub.2 CCH H H CF.sub.3 Ga CH.sub.2 CCH H H CH.sub.2 F Ga CH.sub.2 CCH H H CH.sub.2 Cl Ga CH.sub.2 C CH H H CH.sub.2 Br Gb CH.sub.2 CCH H H CH.sub.2 I Gb CH.sub.2 CCH H H CH.sub.2 OMe Ga CH.sub.2 CCH H H CH.sub.2 OEt Ga CH.sub.2 CCH H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CCH H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CCH H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 CCH H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CCH H H CH.sub.2 SMe Ga CH.sub.2 CCH H H CH.sub.2 SEt Ga CH.sub.2 CCH H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CCH H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 CCH H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CCH H H CH.sub.2 CN Ga CH.sub.2 CCH H H CO.sub.2 Me Ga CH.sub.2 CCH H H CO.sub.2 Et Ga CH.sub.2 CCH H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CCH H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 CCH H H COMe Ga CH.sub.2 CCH H H COEt Ga CH.sub. 2 CCH H H CH.sub.2 COMe Ga CH.sub.2 CCH H H CH.sub.2 COEt Ga CH.sub.2 OMe H H H Ga CH.sub.2 OMe H H Me Gb CH.sub.2 OMe H H Et Gb CH.sub.2 OMe H H Pr-n Gb CH.sub.2 OMe H H Pr-i Gb CH.sub.2 OMe H H Bu-n Gc CH.sub.2 OMe Me H H Ga CH.sub.2 OMe Et H H Gb CH.sub.2 OMe Me H Me Gb CH.sub.2 OMe Me H Et Gb CH.sub.2 OMe H Me Me Ga CH.sub.2 OMe H Me Et Gb CH.sub.2 OMe H H F Ga CH.sub.2 OMe H H Cl Ga CH.sub.2 OMe H H Br Gb

CH.sub.2 OMe H H I Gb CH.sub.2 OMe H H CF.sub.3 Ga CH.sub.2 OMe H H CH.sub.2 F Ga CH.sub.2 OMe H H CH.sub.2 Cl Ga CH.sub.2 OMe H H CH.sub.2 Br Gb CH.sub.2 OMe H H CH.sub.2 I Gb CH.sub.2 OMe H H CH.sub.2 CH.sub.2 F Ga CH.sub.2 OMe H H CH.sub.2 CH.sub.2 Cl Ga CH.sub.2 OMe H H CH.sub.2 CH.sub.2 Br Gb CH.sub.2 OMe H H CH.sub.2 CH.sub.2 I Gb CH.sub.2 OMe H H CH(CH.sub.3)CH.sub.2 F Ga CH.sub.2 OMe H H CH(CH.sub.3)CH.sub.2 Cl Ga CH.sub.2 OMe H H CH(CH.sub.3)CH.sub.2 Br Gb CH.sub.2 OMe H H CH(CH.sub.3)CH.sub.2 I Gb CH.sub.2 OMe H H CH.sub.2 OMe Ga CH.sub.2 OMe H H CH.sub.2 OEt Ga CH.sub.2 OMe H H CH.sub.2 CH.sub.2 OMe Ga CH.sub.2 OMe H H CH.sub.2 CH.sub.2 OEt Ga CH.sub.2 OMe H H CH(CH.sub.3)CH.sub.2 OMe Gb CH.sub.2 OMe H H CH(CH.sub.3)CH.sub.2 OEt Gb CH.sub.2 OMe H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 OMe H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 OMe H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 OMe H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 OMe H H CH.sub.2 SMe Ga CH.sub.2 OMe H H CH.sub.2 SEt Ga CH.sub.2 OMe H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 OMe H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 OMe H H CH.sub.2 CF.sub.3 Ga CH.sub.2 OMe H H CH.sub.2 CN Ga CH.sub.2 OMe H H CO.sub.2 Me Ga CH.sub.2 OMe H H CO.sub.2 Et Ga CH.sub.2 OMe H H CO.sub.2 Pr-n Gb CH.sub.2 OMe H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 OMe H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 OMe H H CH.sub.2 CO.sub.2 Pr-n Gb CH.sub.2 OMe H H COMe Ga CH.sub.2 OMe H H COEt Ga CH.sub.2 OMe H H COPr-n Gb CH.sub.2 OMe H H CH.sub.2 COMe Ga CH.sub.2 OMe H H CH.sub.2 COEt Ga CH.sub.2 OEt H H H Ga CH.sub.2 OEt H H Me Gb CH.sub.2 OEt H H Et Gb CH.sub.2 OEt Me H H Ga CH.sub.2 OEt Et H H Gb CH.sub.2 OEt Me H Me Gb CH.sub.2 OEt Me H Et Gb CH.sub.2 OEt H Me Me Ga CH.sub.2 OEt H Me Et Gb CH.sub.2 OEt H H CF.sub.3 Ga CH.sub.2 OEt H H CH.sub.2 F Ga CH.sub.2 OEt H H CH.sub.2 Cl Ga CH.sub.2 OEt H H CH.sub.2 Br Gb CH.sub.2 OEt H H CH.sub.2 I Gb CH.sub.2 OEt H H CH.sub.2 OMe Ga CH.sub.2 OEt H H CH.sub.2 OEt Ga CH.sub.2 OEt H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 OEt H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 OEt H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 OEt H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 OEt H H CH.sub.2 SMe Ga CH.sub.2 OEt H H CH.sub.2 SEt Ga CH.sub.2 OEt H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 OEt H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 OEt H H CH.sub.2 CF.sub.3 Ga CH.sub.2 OEt H H CH.sub.2 CN Ga CH.sub.2 OEt H H CO.sub.2 Me Ga CH.sub.2 OEt H H CO.sub.2 Et Ga CH.sub.2 OEt H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 OEt H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 OEt H H COMe Ga CH.sub.2 OEt H H COEt Ga CH.sub.2 OEt H H CH.sub.2 COMe Ga CH.sub.2 OEt H H CH.sub.2 COEt Ga CH.sub.2 CH.sub.2 OMe H H H Ga CH.sub.2 CH.sub.2 OMe H H Me Gb CH.sub.2 CH.sub.2 OMe H H Et Gb CH.sub.2 CH.sub.2 OMe Me H H Ga CH.sub.2 CH.sub.2 OMe Et H H Gb CH.sub.2 CH.sub.2 OMe Me H Me Gb CH.sub.2 CH.sub.2 OMe Me H Et Gb CH.sub.2 CH.sub.2 OMe H Me Me Ga CH.sub.2 CH.sub.2 OMe H Me Et Gb CH.sub.2 CH.sub.2 OMe H H CF.sub.3 Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 F Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 Cl Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 Cl Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 Br Gb CH.sub.2 CH.sub.2 OMe H H CH.sub.2 I Gb CH.sub.2 CH.sub.2 OMe H H CH.sub.2 OMe Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 OEt Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 SMe Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 SEt Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 CN Ga CH.sub.2 CH.sub.2 OMe H H CO.sub.2 Me Ga CH.sub.2 CH.sub.2 OMe H H CO.sub.2 Et Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 CH.sub.2 OMe H H COMe Ga CH.sub.2 CH.sub.2 OMe

H H COEt Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 COMe Ga CH.sub.2 CH.sub.2 OMe H H CH.sub.2 COEt Ga CH.sub.2 CH.sub.2 OEt H H H Ga CH.sub.2 CH.sub.2 OEt H H Me Gb CH.sub.2 CH.sub.2 OEt Me H H Ga CH.sub.2 CH.sub.2 OEt Me H Me Gb CH.sub.2 CH.sub.2 OEt H Me Me Ga CH.sub.2 CH.sub.2 OEt H H CF.sub.3 Ga CH.sub.2 CH.sub.2 OEt H H CH.sub.2 F Ga CH.sub.2 CH.sub.2 OEt H H CH.sub.2 Cl Ga CH.sub.2 CH.sub.2 OEt H H CH.sub.2 Br Gb CH.sub.2 CH.sub.2 OEt H H CH.sub.2 I Gb CH.sub.2 CH.sub.2 OEt H H CH.sub.2 OMe Ga CH.sub.2 CH.sub.2 OEt H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CH.sub.2 OEt H H CH.sub.2 OCH.sub.2 C CH Ga CH.sub.2 CH.sub.2 OEt H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 CH.sub.2 OEt H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CH.sub.2 OEt H H CH.sub.2 SMe Ga CH.sub.2 CH.sub.2 OEt H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CH.sub.2 OEt H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CH.sub.2 OEt H H CH.sub.2 CN Ga CH.sub.2 CH.sub.2 OEt H H CO.sub.2 Me Ga CH.sub.2 CH.sub.2 OEt H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CH.sub.2 OEt H H COMe Ga CH.sub.2 CH.sub.2 OEt H H CH.sub.2 COMe Ga CH(CH.sub.3)CH.sub.2 OMe H H H Ga CH(CH.sub.3)CH.sub.2 OMe H H Me Gb CH(CH.sub.3)CH.sub.2 OMe H H Et Gb CH(CH.sub.3)CH.sub.2 OMe Me H H Ga CH(CH.sub.3)CH.sub.2 OMe Et H H Gb CH(CH.sub.3)CH.sub.2 OMe Me H Me Gb CH(CH.sub.3)CH.sub.2 OMe Me H Et Gb CH(CH.sub.3)CH.sub.2 OMe H Me Me Ga CH(CH.sub.3)CH.sub.2 OMe H Me Et Gb CH(CH.sub.3 )CH.sub.2 OMe H H CF.sub.3 Ga CH(CH.sub.3)CH.sub.2 OMe

H H CH.sub.2 F Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 Cl Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 Br Gb CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 I Gb CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 OMe Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 OEt Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 OCH.sub.2 CCH Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 OCHF.sub.2 Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 OCF.sub.3 Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 SMe Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 SEt Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 SO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 SO.sub.2 Et Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 CF.sub.3 Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 CN Ga CH(CH.sub.3)CH.sub.2 OMe H H CO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 OMe H H CO.sub.2 Et Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 CO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 CO.sub.2 Et Ga CH(CH.sub.3)CH.sub.2 OMe H H COMe Ga CH(CH.sub.3)CH.sub.2 OMe H H COEt Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 COMe Ga CH(CH.sub.3)CH.sub.2 OMe H H CH.sub.2 COEt Ga CH(CH.sub.3)CH.sub.2 OEt H H H Ga CH(CH.sub.3)CH.sub.2 OEt H H Me Gb CH(CH.sub.3)CH.sub.2 OEt Me H H Ga CH(CH.sub.3)CH.sub.2 OEt Me H Me Gb CH(CH.sub.3)CH.sub.2 OEt H Me Me Ga CH(CH.sub.3)CH.sub.2 OEt H H CF.sub.3 Ga CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 F Ga CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 Cl Ga CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 Br Gb CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 I Gb CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 OMe Ga CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 OCH.sub.2 CCH Ga CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 OCHF.sub.2 Ga CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 OCF.sub.3 Ga CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 SMe Ga CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 SO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 CF.sub.3 Ga CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 CN Ga CH(CH.sub.3)CH.sub.2 OEt H H CO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 CO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 OEt H H COMe Ga CH(CH.sub.3)CH.sub.2 OEt H H CH.sub.2 COMe Ga CH.sub.2 OCHF.sub.2 H H H Ga CH.sub.2 OCHF.sub.2 H H Me Gb CH.sub.2 OCHF.sub.2 H H Et Gb CH.sub.2 OCHF.sub.2 H H Pr-n Gb CH.sub.2 OCHF.sub.2 H H Pr-i Gb CH.sub.2 OCHF.sub.2 H H Bu-n Gc CH.sub.2 OCHF.sub.2 Me H H Ga CH.sub.2 OCHF.sub.2 Et H H Gb CH.sub.2 OCHF.sub.2 Me H Me Gb CH.sub.2 OCHF.sub.2 Me H Et Gb CH.sub.2 OCHF.sub.2 H Me Me Ga CH.sub.2 OCHF.sub.2 H Me Et Gb CH.sub.2 OCHF.sub.2 H H F Ga CH.sub.2 OCHF.sub.2 H H Cl Ga CH.sub.2 OCHF.sub.2 H H Br Gb CH.sub.2 OCHF.sub.2 H H I Gb CH.sub.2 OCHF.sub.2 H H CF.sub.3 Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 F Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 Cl Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 Br Gb CH.sub.2 OCHF.sub.2 H H CH.sub.2 I Gb CH.sub.2 OCHF.sub.2 H H CH.sub.2 CH.sub.2 F Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 CH.sub.2 Cl Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 CH.sub.2 Br Gb CH.sub.2 OCHF.sub.2 H H CH.sub.2 CH.sub.2 I Gb CH.sub.2 OCHF.sub.2 H H CH(CH.sub.3)CH.sub.2 F Ga CH.sub.2 OCHF.sub. 2 H H CH(CH.sub.3)CH.sub.2 Cl Ga CH.sub.2 OCHF.sub.2 H H CH(CH.sub.3)CH.sub.2 Br Gb CH.sub.2 OCHF.sub.2 H H CH(CH.sub.3)CH.sub.2 I Gb CH.sub.2 OCHF.sub.2 H H CH.sub.2 OMe Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 OEt Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 CH.sub.2 OMe Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 CH.sub.2 OEt Ga CH.sub.2 OCHF.sub.2 H H CH(CH.sub.3)CH.sub.2 OMe Gb CH.sub.2 OCHF.sub.2 H H CH(CH.sub.3)CH.sub.2 OEt Gb CH.sub.2 OCHF.sub.2 H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 SMe Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 SEt Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 SO.sub. 2 Et Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 CF.sub.3 Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 CN Ga CH.sub.2 OCHF.sub.2 H H CO.sub.2 Me Ga CH.sub.2 OCHF.sub.2 H H CO.sub.2 Et Ga CH.sub.2 OCHF.sub.2 H H CO.sub.2 Pr-n Gb CH.sub.2 OCHF.sub.2 H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 CO.sub.2 Pr-n Gb CH.sub.2 OCHF.sub.2 H H COMe Ga CH.sub.2 OCHF.sub.2 H H COEt Gb CH.sub.2 OCHF.sub.2 H H COPr-n Gb CH.sub.2 OCHF.sub.2 H H CH.sub.2 COMe Ga CH.sub.2 OCHF.sub.2 H H CH.sub.2 COEt Ga CH.sub.2 SMe H H H Ga CH.sub.2 SMe H H Me Gb CH.sub.2 SMe H H Et Gb CH.sub.2 SMe H H Pr-n Gb CH.sub.2 SMe H H Pr-i Gb

CH.sub.2 SMe H H Bu-n Gc CH.sub.2 SMe Me H H Ga CH.sub.2 SMe Et H H Gb CH.sub.2 SMe Me H Me Gb CH.sub.2 SMe Me H Et Gb CH.sub.2 SMe H Me Me Ga CH.sub.2 SMe H Me Et Gb CH.sub.2 SMe H H F Ga CH.sub.2 SMe H H Cl Ga CH.sub.2 SMe H H Br Gb CH.sub.2 SMe H H I Gb CH.sub.2 SMe H H CF.sub.3 Ga CH.sub.2 SMe H H CH.sub.2 F Ga CH.sub.2 SMe H H CH.sub.2 Cl Ga CH.sub.2 SMe H H CH.sub.2 Br Gb CH.sub.2 SMe H H CH.sub.2 I Gb CH.sub.2 SMe H H CH.sub.2 CH.sub.2 F Ga CH.sub.2 SMe H H CH.sub.2 CH.sub.2 Cl Ga CH.sub.2 SMe H H CH.sub.2 CH.sub.2 Br Gb CH.sub.2 SMe H H CH.sub.2 CH.sub.2 I Gb CH.sub.2 SMe H H CH(CH.sub.3)CH.sub.2 F Ga CH.sub.2 SMe H H CH(CH.sub.3)CH.sub.2 Cl Ga CH.sub.2 SMe H H CH(CH.sub.3)CH.sub.2 Br Gb CH.sub.2 SMe H H CH(CH.sub.3)CH.sub.2 I Gb CH.sub.2 SMe H H CH.sub.2 OMe Ga CH.sub.2 SMe H H CH.sub.2 OEt Ga CH.sub.2 SMe H H CH.sub.2 CH.sub.2 OMe Ga CH.sub.2 SMe H H CH.sub.2 CH.sub.2 OEt Ga CH.sub.2 SMe H H CH(CH.sub.3)CH.sub.2 OMe Gb CH.sub.2 SMe H H CH(CH.sub.3)CH.sub.2 OEt Gb CH.sub.2 SMe H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 SMe H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 SMe H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 SMe H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 SMe H H CH.sub.2 SMe Ga CH.sub.2 SMe H H CH.sub.2 SEt Ga CH.sub.2 SMe H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 SMe H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 SMe H H CH.sub.2 CF.sub.3 Ga CH.sub.2 SMe H H CH.sub.2 CN Ga CH.sub.2 SMe H H CO.sub.2 Me Ga CH.sub.2 SMe H H CO.sub.2 Et Ga CH.sub.2 SMe H H CO.sub.2 Pr-n Gb CH.sub.2 SMe H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 SMe H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 SMe H H CH.sub.2 CO.sub.2 Pr-n Gb CH.sub.2 SMe H H COMe Ga CH.sub.2 SMe H H COEt Ga CH.sub.2 SMe H H COPr-n Gb CH.sub.2 SMe H H CH.sub.2 COMe Ga CH.sub.2 SMe H H CH.sub.2 COEt Ga CH.sub.2 SEt H H H Ga CH.sub.2 SEt H H Me Gb CH.sub.2 SEt H H Et Gb CH.sub.2 SEt Me H H Ga CH.sub.2 SEt Et H H Gb CH.sub.2 SEt Me H Me Gb CH.sub.2 SEt Me H Et Gb CH.sub.2 SEt H Me Me Ga CH.sub.2 SEt H Me Et Gb CH.sub.2 SEt H H CF.sub.3 Ga CH.sub.2 SEt H H CH.sub.2 F Ga CH.sub.2 SEt H H CH.sub.2 Cl Ga CH.sub.2 SEt H H CH.sub.2 Br Gb CH.sub.2 SEt H H CH.sub.2 I Gb CH.sub.2 SEt H H CH.sub.2 OMe Ga CH.sub.2 SEt H H CH.sub.2 OEt Ga CH.sub.2 SEt H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 SEt H H CH.sub.2 OCH.sub.2 C CH Ga CH.sub.2 SEt H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 SEt H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 SEt H H CH.sub.2 SMe Ga CH.sub.2 SEt H H CH.sub.2 SEt Ga CH.sub.2 SEt H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 SEt H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 SEt H H CH.sub.2 CF.sub.3 Ga CH.sub.2 SEt H H CH.sub.2 CN Ga CH.sub.2 SEt H H CO.sub.2 Me Ga CH.sub.2 SEt H H CO.sub.2 Et Ga CH.sub.2 SEt H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 SEt H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 SEt H H COMe Ga CH.sub.2 SEt H H COEt Ga CH.sub.2 SEt H H CH.sub.2 COMe Ga CH.sub.2 SEt H H CH.sub.2 COEt Ga CH.sub.2 SEt H H CH.sub.2 COMe Ga CH.sub.2 SEt H H CH.sub.2 COEt Ga CH.sub.2 SO.sub.2 Me H H H Ga CH.sub.2 SO.sub.2 Me H H Me Gb CH.sub.2 SO.sub.2 Me H H Et Gb CH.sub.2 SO.sub.2 Me H H Pr-n Gb CH.sub.2 SO.sub.2 Me H H Pr-i Gb CH.sub.2 SO.sub.2 Me H H Bu-n Gc CH.sub.2 SO.sub.2 Me Me H H Ga CH.sub.2 SO.sub.2 Me Et H H Gb CH.sub.2 SO.sub.2 Me Me H Me Gb CH.sub.2 SO.sub.2 Me Me H Et Gb CH.sub.2 SO.sub.2 Me H Me Me Ga CH.sub.2 SO.sub.2 Me H Me Et Gb CH.sub.2 SO.sub.2 Me H H F Ga CH.sub.2 SO.sub.2 Me H H Cl Ga CH.sub.2 SO.sub.2 Me H H Br Gb CH.sub.2 SO.sub.2 Me H H I Gb CH.sub.2 SO.sub.2 Me H H CF.sub.3 Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 F Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 Cl Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 Br Gb CH.sub.2 SO.sub.2 Me H H CH.sub.2 I Gb CH.sub.2 SO.sub.2 Me H H CH.sub.2 CH.sub.2 F Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 CH.sub.2 Cl Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 CH.sub.2 Br

Gb CH.sub.2 SO.sub.2 Me H H CH.sub.2 CH.sub.2 I Gb CH.sub.2 SO.sub.2 Me H H CH(CH.sub.3)CH.sub.2 F Ga CH.sub.2 SO.sub.2 Me H H CH(CH.sub.3)CH.sub.2 Cl Ga CH.sub.2 SO.sub.2 Me H H CH(CH.sub.3)CH.sub.2 Br Gb CH.sub.2 SO.sub.2 Me H H CH(CH.sub.3)CH.sub.2 I Gb CH.sub.2 SO.sub.2 Me H H CH.sub.2 OMe Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 OEt Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 CH.sub.2 OMe Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 CH.sub.2 OEt Ga CH.sub.2 SO.sub.2 Me H H CH(CH.sub.3)CH.sub.2 OMe Gb CH.sub.2 SO.sub.2 Me H H CH(CH.sub.3)CH.sub.2 OEt Gb CH.sub.2 SO.sub.2 Me H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 OCF.sub.3 Ga CH.sub. 2 SO.sub.2 Me H H CH.sub.2 SMe Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 SEt Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 CF.sub.3 Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 CN Ga CH.sub.2 SO.sub.2 Me H H CO.sub.2 Me Ga CH.sub.2 SO.sub.2 Me H H CO.sub.2 Et Ga CH.sub.2 SO.sub.2 Me H H CO.sub.2 Pr-n Gb CH.sub.2 SO.sub.2 Me H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 CO.sub.2 Pr-n Gb CH.sub.2 SO.sub.2 Me H H COMe Ga CH.sub.2 SO.sub.2 Me H H COEt Ga CH.sub.2 SO.sub.2 Me H H COPr-n Gb CH.sub.2 SO.sub.2 Me H H CH.sub.2 COMe Ga CH.sub.2 SO.sub.2 Me H H CH.sub.2 COEt Ga CH.sub.2 SO.sub.2 Et H H H Ga CH.sub.2 SO.sub.2 Et H H Me Gb CH.sub.2 SO.sub.2 Et H H Et Gb CH.sub.2 SO.sub.2 Et Me H H Ga CH.sub.2 SO.sub.2 Et Et H H Gb CH.sub.2 SO.sub.2 Et Me H Me Gb CH.sub.2 SO.sub.2 Et Me H Et Gb CH.sub.2 SO.sub.2 Et H Me Me Ga CH.sub.2 SO.sub.2 Et H Me Et Gb CH.sub.2 SO.sub.2 Et H H CF.sub.3 Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 F Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 Cl Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 Br Gb CH.sub.2 SO.sub.2 Et H H CH.sub.2 I Gb CH.sub.2 SO.sub.2 Et H H CH.sub.2 OMe Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 OEt Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 SMe Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 SEt Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 CF.sub.3 Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 CN Ga CH.sub.2 SO.sub.2 Et H H CO.sub.2 Me Ga CH.sub.2 SO.sub.2 Et H H CO.sub.2 Et Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 SO.sub.2 Et H H COMe Ga CH.sub.2 SO.sub.2 Et H H COEt Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 COMe Ga CH.sub.2 SO.sub.2 Et H H CH.sub.2 COEt Ga CH.sub.2 F H H H Ga CH.sub.2 F H H Me Gb CH.sub.2 F H H Et Gb CH.sub.2 F H H Pr-n Gb CH.sub.2 F H H Pr-i Gb CH.sub.2 F H H Bu-n Gc CH.sub.2 F Me H H Ga CH.sub.2 F Et H H Gb CH.sub.2 F Me H Me Gb CH.sub.2 F Me H Et Gb CH.sub.2 F H Me Me Ga CH.sub.2 F H Me Et Gb CH.sub.2 F H H F Ga CH.sub.2 F H H Cl Ga CH.sub.2 F H H Br Gb CH.sub.2 F H H I Gb CH.sub.2 F H H CF.sub.3 Ga CH.sub.2 F H H CH.sub.2 F Ga CH.sub.2 F H H CH.sub.2 Cl Ga CH.sub.2 F H H CH.sub.2 Br Gb CH.sub.2 F H H CH.sub.2 I Gb CH.sub.2 F H H CH.sub.2 CH.sub.2 F Ga CH.sub.2 F H H CH.sub.2 CH.sub.2 Cl Ga CH.sub.2 F H H CH.sub.2 CH.sub.2 Br Gb CH.sub.2 F H H CH.sub.2 CH.sub.2 I Gb CH.sub.2 F H H CH(CH.sub.3)CH.sub.2 F Ga CH.sub.2 F H H CH(CH.sub.3)CH.sub.2 Cl Ga CH.sub.2 F H H CH(CH.sub.3)CH.sub.2 Br Gb CH.sub.2 F H H CH(CH.sub.3)CH.sub.2 I Gb CH.sub.2 F H H CH.sub.2 OMe Ga CH.sub.2 F H H CH.sub.2 OEt Ga CH.sub.2 F H H CH.sub.2 CH.sub.2 OMe Ga CH.sub.2 F H H CH.sub.2 CH.sub.2 OEt Ga CH.sub.2 F H H CH(CH.sub.3)CH.sub.2 OMe Gb CH.sub.2 F H H CH(CH.sub.3)CH.sub.2 OEt Gb CH.sub.2 F H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 F H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 F H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 F H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 F H H CH.sub.2 SMe Ga CH.sub.2 F H H CH.sub.2 SEt Ga CH.sub.2 F H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 F H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 F H H CH.sub.2 CF.sub.3 Ga CH.sub.2 F H H CH.sub.2 CN Ga CH.sub.2 F H H CO.sub.2 Me Ga CH.sub.2 F H H CO.sub.2 Et Ga CH.sub.2 F H H CO.sub.2 Pr-n Gb CH.sub.2 F H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 F H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 F H H CH.sub.2 CO.sub.2 Pr-n Gb CH.sub.2 F H H COMe Ga CH.sub.2 F H H COEt Ga CH.sub.2 F H H COPr-n Gb CH.sub.2 F H H CH.sub.2 COMe Ga CH.sub.2 F H H CH.sub.2 COEt Ga CH.sub.2 Cl H H H Ga CH.sub.2 Cl H H Me Gb CH.sub.2 Cl H H Et Gb CH.sub.2 Cl H H Pr-n Gb CH.sub.2 Cl H H Pr-i Gb CH.sub.2 Cl H H Bu-n Gc CH.sub.2 Cl Me H H Ga CH.sub.2 Cl Et H H Gb CH.sub.2 Cl Me H Me Gb CH.sub.2 Cl Me H Et Gb CH.sub.2 Cl H Me Me Ga CH.sub.2 Cl H Me Et Gb CH.sub.2 Cl H H F Ga CH.sub.2 Cl H H Cl Ga CH.sub.2 Cl H H Br Gb

CH.sub.2 Cl H H I Gb CH.sub. 2 Cl H H CF.sub.3 Ga CH.sub.2 Cl H H CH.sub.2 F Ga CH.sub.2 Cl H H CH.sub.2 Cl Ga CH.sub.2 Cl H H CH.sub.2 Br Gb CH.sub.2 Cl H H CH.sub.2 I Gb CH.sub.2 Cl H H CH.sub.2 CH.sub.2 F Ga CH.sub.2 Cl H H CH.sub.2 CH.sub.2 Cl Ga CH.sub.2 Cl H H CH.sub.2 CH.sub.2 Br Gb CH.sub.2 Cl H H CH.sub.2 CH.sub.2 I Gb CH.sub.2 Cl H H CH(CH.sub.3)CH.sub.2 F Ga CH.sub.2 Cl H H CH(CH.sub.3)CH.sub.2 Cl Ga CH.sub.2 Cl H H CH(CH.sub.3)CH.sub.2 Br Gb CH.sub.2 Cl H H CH(CH.sub.3)CH.sub.2 I Gb CH.sub.2 Cl H H CH.sub.2 OMe Ga CH.sub.2 Cl H H CH.sub.2 OEt Ga CH.sub.2 Cl H H CH.sub.2 CH.sub.2 OMe Ga CH.sub.2 Cl H H CH.sub.2 CH.sub.2 OEt Ga CH.sub.2 Cl H H CH(CH.sub.3)CH.sub.2 OMe Gb CH.sub.2 Cl H H CH(CH.sub.3)CH.sub. 2 OEt Gb CH.sub.2 Cl H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 Cl H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 Cl H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 Cl H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 Cl H H CH.sub.2 SMe Ga CH.sub.2 Cl H H CH.sub.2 SEt Ga CH.sub.2 Cl H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 Cl H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 Cl H H CH.sub.2 CF.sub.3 Ga CH.sub.2 Cl H H CH.sub.2 CN Ga CH.sub.2 Cl H H CO.sub.2 Me Ga CH.sub.2 Cl H H CO.sub.2 Et Ga CH.sub.2 Cl H H CO.sub.2 Pr-n Gb CH.sub.2 Cl H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 Cl H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 Cl H H CH.sub.2 CO.sub.2 Pr-n Gb CH.sub.2 Cl H H COMe Ga CH.sub.2 Cl H H COEt Ga CH.sub.2 Cl H H COPr-n Gb CH.sub.2 Cl H H CH.sub.2 COMe Ga CH.sub.2 Cl H H CH.sub.2 COEt Ga CH.sub.2 Br H H H Ga CH.sub.2 Br H H Me Gb CH.sub.2 Br H H Et Gb CH.sub.2 Br Me H H Ga CH.sub.2 Br Et H H Gb CH.sub.2 Br Me H Me Gb CH.sub.2 Br Me H Et Gb CH.sub.2 Br H Me Me Ga CH.sub.2 Br H Me Et Gb CH.sub.2 Br H H CF.sub.3 Ga CH.sub.2 Br H H CH.sub.2 F Ga CH.sub.2 Br H H CH.sub.2 Cl Ga CH.sub.2 Br H H CH.sub.2 Br Gb CH.sub.2 Br H H CH.sub.2 I Gb CH.sub.2 Br H H CH.sub.2 OMe Ga CH.sub.2 Br H H CH.sub.2 OEt Ga CH.sub.2 Br H H CH.sub.2 OCH.sub.2 CHCH.sub.2

Ga CH.sub.2 Br H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 Br H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 Br H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 Br H H CH.sub.2 SMe Ga CH.sub.2 Br H H CH.sub.2 SEt Ga CH.sub.2 Br H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 Br H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 Br H H CH.sub.2 CF.sub.3 Ga CH.sub.2 Br H H CH.sub.2 CN Ga CH.sub.2 Br H H CO.sub.2 Me Ga CH.sub.2 Br H H CO.sub.2 Et Ga CH.sub.2 Br H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 Br H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 Br H H COMe Ga CH.sub.2 Br H H COEt Ga CH.sub.2 Br H H CH.sub.2 COMe Ga CH.sub.2 Br H H CH.sub.2 COEt Ga CH.sub.2 I H H H Ga CH.sub.2 I H H Me Gb CH.sub.2 I H H Et Gb CH.sub.2 I Me H H Ga CH.sub.2 I Et H H Gb CH.sub.2 I Me H Me Gb CH.sub.2 I Me H Et Gb CH.sub.2 I H Me Me Ga CH.sub.2 I H Me Et Gb CH.sub.2 I H H CF.sub.3 Ga CH.sub.2 I H H CH.sub.2 F Ga CH.sub.2 I H H CH.sub.2 Cl Ga CH.sub.2 I H H CH.sub.2 Br Gb CH.sub.2 I H H CH.sub.2 I Gb CH.sub.2 I H H CH.sub.2 OMe Ga CH.sub.2 I H H CH.sub.2 OEt Ga CH.sub.2 I H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 I H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 I H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 I H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 I H H CH.sub.2 SMe Ga CH.sub.2 I H H CH.sub.2 SEt Ga CH.sub.2 I H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 I H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 I H H CH.sub.2 CF.sub.3 Ga CH.sub.2 I H H CH.sub.2 CN Ga CH.sub.2 I H H CO.sub.2 Me Ga CH.sub.2 I H H CO.sub.2 Et Ga CH.sub.2 I H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 I H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 I H H COMe Ga CH.sub.2 I H H COEt Ga CH.sub.2 I H H CH.sub.2 COMe Ga CH.sub.2 I H H CH.sub.2 COEt Ga CH.sub.2 CH.sub.2 F H H H Ga CH.sub.2 CH.sub.2 F H H Me Gb CH.sub.2 CH.sub.2 F H H Et Gb CH.sub.2 CH.sub.2 F Me H H Ga CH.sub.2 CH.sub.2 F Et H H Gb CH.sub.2 CH.sub.2 F Me H Me Gb CH.sub.2 CH.sub.2 F Me H Et Gb CH.sub.2 CH.sub.2 F H Me Me Ga CH.sub.2 CH.sub.2 F H Me Et Gb CH.sub.2 CH.sub.2 F H H CF.sub.3 Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 F Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 Cl Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 Br Gb CH.sub.2 CH.sub.2 F H H CH.sub.2 I Gb CH.sub.2 CH.sub.2 F H H CH.sub.2 OMe Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 OEt Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CH.sub. 2 F H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 SMe Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 SEt Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 CN Ga CH.sub.2 CH.sub.2 F H H CO.sub.2 Me Ga CH.sub.2 CH.sub.2 F H H CO.sub.2 Et Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 CH.sub.2 F H H COMe Ga CH.sub.2 CH.sub.2 F H H COEt Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 COMe Ga CH.sub.2 CH.sub.2 F H H CH.sub.2 COEt Ga CH.sub.2 CH.sub.2 Cl H H H Ga CH.sub.2 CH.sub.2 Cl H H Me Gb CH.sub.2 CH.sub.2 Cl H H Et Gb CH.sub.2 CH.sub.2 Cl Me H H Ga CH.sub.2 CH.sub.2 Cl Et H H Gb CH.sub.2 CH.sub.2 Cl Me H Me Gb CH.sub.2 CH.sub.2 Cl Me H Et Gb CH.sub.2 CH.sub.2 Cl H Me Me Ga CH.sub.2 CH.sub.2 Cl H Me Et Gb CH.sub.2 CH.sub.2 Cl H H CF.sub.3 Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 F Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 Cl Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 Br Gb CH.sub.2 CH.sub.2 Cl H H CH.sub.2 I Gb CH.sub.2 CH.sub.2 Cl H H CH.sub.2 OMe Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 OEt Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CH.sub. 2 Cl H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 SMe Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 SEt Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 CN Ga CH.sub.2 CH.sub.2 Cl H H CO.sub.2 Me Ga CH.sub.2 CH.sub.2 Cl H H CO.sub.2 Et Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 CH.sub.2 Cl H H COMe Ga CH.sub.2 CH.sub.2 Cl H H COEt Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 COMe Ga CH.sub.2 CH.sub.2 Cl H H CH.sub.2 COEt Ga CH.sub.2 CH.sub.2 Br H H H Ga CH.sub.2 CH.sub.2 Br H H Me Gb CH.sub.2 CH.sub.2 Br Me H H Ga CH.sub.2 CH.sub.2 Br Me H Me Gb CH.sub.2 CH.sub.2 Br H Me Me Ga CH.sub.2 CH.sub.2 Br H H CF.sub.3 Ga CH.sub.2 CH.sub.2 Br H H CH.sub.2 F Ga CH.sub.2 CH.sub.2 Br H H CH.sub.2 Cl Ga CH.sub.2 CH.sub.2 Br H H CH.sub.2 Br Gb CH.sub.2 CH.sub.2 Br H H CH.sub.2 I Gb CH.sub.2 CH.sub.2 Br H H CH.sub.2 OMe Ga CH.sub.2 CH.sub.2 Br H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CH.sub.2 Br H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CH.sub.2 Br H H CH.sub.2 OCHF.sub.2

Ga CH.sub.2 CH.sub.2 Br H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CH.sub.2 Br H H CH.sub.2 SMe Ga CH.sub.2 CH.sub.2 Br H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CH.sub.2 Br H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CH.sub.2 Br H H CH.sub.2 CN Ga CH.sub. 2 CH.sub.2 Br H H CO.sub.2 Me Ga CH.sub.2 CH.sub.2 Br H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CH.sub.2 Br H H COMe Ga CH.sub.2 CH.sub.2 Br H H CH.sub.2 COMe Ga CH.sub.2 CH.sub.2 I H H H Ga CH.sub.2 CH.sub.2 I H H Me Gb CH.sub.2 CH.sub.2 I Me H H Ga CH.sub.2 CH.sub.2 I Me H Me Gb CH.sub.2 CH.sub.2 I H Me Me Ga CH.sub.2 CH.sub.2 I H H CF.sub.3 Ga CH.sub.2 CH.sub.2 I H H CH.sub.2 F Ga CH.sub.2 CH.sub.2 I H H CH.sub.2 Cl Ga CH.sub.2 CH.sub.2 I H H CH.sub.2 Br Gb CH.sub.2 CH.sub.2 I H H CH.sub.2 I Gb CH.sub.2 CH.sub.2 I H H CH.sub.2 OMe Ga CH.sub.2 CH.sub.2 I H H CH.sub.2 OCH.sub.2 CH CH.sub.2 Ga CH.sub.2 CH.sub.2 I H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CH.sub.2 I H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 CH.sub.2 I H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CH.sub.2 I H H CH.sub.2 SMe Ga CH.sub.2 CH.sub.2 I H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CH.sub.2 I H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CH.sub.2 I H H CH.sub.2 CN Ga CH.sub.2 CH.sub.2 I H H CO.sub.2 Me Ga CH.sub.2 CH.sub.2 I H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CH.sub.2 I H H COMe Ga CH.sub.2 CH.sub.2 I H H CH.sub.2 COMe Ga CH(CH.sub.3)CH.sub.2 F H H H Ga CH(CH.sub.3)CH.sub.2 F H H Me Gb CH(CH.sub.3)CH.sub.2 F H H Et Gb CH(CH.sub.3)CH.sub.2 F Me H H Ga CH(CH.sub.3)CH.sub.2 F Et H H Gb CH(CH.sub.3)CH.sub.2 F Me H Me Gb CH(CH.sub.3)CH.sub.2 F Me H Et Gb CH(CH.sub.3)CH.sub.2 F H Me Me Ga CH(CH.sub.3)CH.sub.2 F H Me Et Gb CH(CH.sub.3)CH.sub.2 F H H CF.sub.3 Ga CH(CH.sub.3)CH.sub. 2 F H H CH.sub.2 F Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 Cl Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 Br Gb CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 I Gb CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 OMe Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 OEt Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 OCH.sub.2 CCH Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 OCHF.sub.2 Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 OCF.sub.3 Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 SMe Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 SEt Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 SO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 SO.sub.2 Et Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 CF.sub.3 Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 CN Ga CH(CH.sub.3)CH.sub.2 F H H CO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 F H H CO.sub.2 Et Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 CO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 CO.sub.2 Et Ga CH(CH.sub.3)CH.sub.2 F H H COMe Ga CH(CH.sub.3)CH.sub.2 F H H COEt Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 COMe Ga CH(CH.sub.3)CH.sub.2 F H H CH.sub.2 COEt Ga CH(CH.sub.3)CH.sub.2 Cl H H H Ga CH(CH.sub.3)CH.sub.2 Cl H H Me Gb CH(CH.sub.3)CH.sub.2 Cl H H Et Gb CH(CH.sub.3)CH.sub.2 Cl Me H H Ga CH(CH.sub.3)CH.sub.2 Cl Et H H Gb CH(CH.sub.3)CH.sub.2 Cl Me H Me Gb CH(CH.sub.3)CH.sub.2 Cl Me H Et Gb CH(CH.sub.3)CH.sub.2 Cl H Me Me Ga CH(CH.sub.3)CH.sub.2 Cl H Me Et Gb CH(CH.sub.3)CH.sub.2 Cl H H CF.sub.3 Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 F Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 Cl Ga CH(CH.sub.3)CH.sub. 2 Cl H H CH.sub.2 Br Gb CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 I Gb CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 OMe Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 OEt Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 OCH.sub.2 CH CH.sub.2 Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 OCH.sub.2 CCH Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 OCHF.sub.2 Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 OCF.sub.3 Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 SMe Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 SEt Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 SO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 SO.sub.2 Et Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 CF.sub.3 Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 CN Ga CH(CH.sub.3)CH.sub.2 Cl H H CO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 Cl H H CO.sub.2 Et Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 CO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 CO.sub.2 Et Ga CH(CH.sub.3)CH.sub.2 Cl H H COMe Ga CH(CH.sub.3)CH.sub.2 Cl H H COEt Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 COMe Ga CH(CH.sub.3)CH.sub.2 Cl H H CH.sub.2 COEt Ga CH(CH.sub.3)CH.sub.2 Br H H H Ga CH(CH.sub.3)CH.sub.2 Br H H Me Gb CH(CH.sub.3)CH.sub.2 Br Me H H Ga CH(CH.sub.3)CH.sub.2 Br Me H Me Gb CH(CH.sub.3)CH.sub.2 Br H Me Me Ga CH(CH.sub.3)CH.sub.2 Br H H CF.sub.3 Ga CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 F Ga CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 Cl Ga CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 Br Gb CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 I Gb CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 OMe Ga

CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 OCH.sub.2 CCH Ga CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 OCHF.sub.2 Ga CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 OCF.sub.3 Ga CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 SMe Ga CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 SO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 CF.sub.3 Ga CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 CN Ga CH(CH.sub.3)CH.sub.2 Br H H CO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 CO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 Br H H COMe Ga CH(CH.sub.3)CH.sub.2 Br H H CH.sub.2 COMe Ga CH(CH.sub.3)CH.sub.2 I H H H Ga CH(CH.sub.3)CH.sub.2 I H H Me Gb CH(CH.sub.3)CH.sub.2 I Me H H Ga CH(CH.sub.3)CH.sub.2 I Me H Me Gb CH(CH.sub.3)CH.sub.2 I H Me Me Ga CH(CH.sub.3)CH.sub.2 I H H CF.sub.3 Ga CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 F Ga CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 Cl Ga CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 Br Gb CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 I Gb CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 OMe Ga CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 OCH.sub.2 CCH Ga CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 OCHF.sub.2 Ga CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 OCF.sub.3 Ga CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 SMe Ga CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 SO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 CF.sub.3 Ga CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 CN Ga CH(CH.sub.3)CH.sub.2 I H H CO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 CO.sub.2 Me Ga CH(CH.sub.3)CH.sub.2 I H H COMe Ga CH(CH.sub.3)CH.sub.2 I H H CH.sub.2 COMe Ga CH.sub.2 CF.sub. 3 H H H Ga CH.sub.2 CF.sub.3 H H Me Gb CH.sub.2 CF.sub.3 H H Et Gb CH.sub.2 CF.sub.3 H H Pr-n Gb CH.sub.2 CF.sub.3 H H Pr-i Gb CH.sub.2 CF.sub.3 H H Bu-n Gc CH.sub.2 CF.sub.3 Me H H Ga CH.sub.2 CF.sub.3 Et H H Gb CH.sub.2 CF.sub.3 Me H Me Gb CH.sub.2 CF.sub.3 Me H Et Gb CH.sub.2 CF.sub.3 H Me Me Ga CH.sub.2 CF.sub.3 H Me Et Gb CH.sub.2 CF.sub.3 H H F Ga CH.sub.2 CF.sub.3 H H Cl Ga CH.sub.2 CF.sub.3 H H Br Gb CH.sub.2 CF.sub.3 H H I Gb CH.sub.2 CF.sub.3 H H CF.sub.3 Ga CH.sub.2 CF.sub.3 H H CH.sub.2 F Ga CH.sub.2 CF.sub.3 H H CH.sub.2 Cl Ga CH.sub.2 CF.sub.3 H H CH.sub.2 Br Gb CH.sub.2 CF.sub.3 H H CH.sub.2 I Gb CH.sub.2 CF.sub.3 H H CH.sub.2 CH.sub.2 F Ga CH.sub.2 CF.sub.3 H H CH.sub.2 CH.sub.2 Cl Ga CH.sub.2 CF.sub.3 H H CH.sub.2 CH.sub.2 Br Gb CH.sub.2 CF.sub.3 H H CH.sub.2 CH.sub.2 I Gb CH.sub.2 CF.sub.3 H H CH(CH.sub.3)CH.sub.2 F Ga CH.sub.2 CF.sub.3 H H CH(CH.sub.3)CH.sub.2 Cl Ga CH.sub.2 CF.sub.3 H H CH(CH.sub.3)CH.sub.2 Br Gb CH.sub.2 CF.sub.3 H H CH(CH.sub.3)CH.sub.2 I Gb CH.sub.2 CF.sub.3 H H CH.sub.2 OMe Ga CH.sub.2 CF.sub.3 H H CH.sub.2 OEt Ga CH.sub.2 CF.sub.3 H H CH.sub.2 CH.sub.2 OMe Ga CH.sub.2 CF.sub.3 H H CH.sub.2 CH.sub.2 OEt Ga CH.sub.2 CF.sub.3 H H CH(CH.sub.3)CH.sub.2 OMe Gb CH.sub.2 CF.sub.3 H H CH(CH.sub.3)CH.sub.2 OEt Gb CH.sub.2 CF.sub.3 H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CF.sub.3 H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CF.sub.3 H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 CF.sub.3 H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CF.sub.3 H H CH.sub.2 SMe Ga CH.sub.2 CF.sub.3 H H CH.sub.2 SEt Ga CH.sub.2 CF.sub.3 H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CF.sub.3 H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 CF.sub.3 H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CF.sub.3 H H CH.sub.2 CN Ga CH.sub.2 CF.sub.3 H H CO.sub.2 Me Ga CH.sub.2 CF.sub.3 H H CO.sub.2 Et Ga CH.sub.2 CF.sub.3 H H CO.sub.2 Pr-n Gb CH.sub.2 CF.sub.3 H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CF.sub.3 H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 CF.sub.3 H H CH.sub.2 CO.sub.2 Pr-n Gb CH.sub.2 CF.sub.3 H H COMe Ga CH.sub.2 CF.sub.3 H H COEt Ga CH.sub.2 CF.sub.3 H H COPr-n Gb CH.sub.2 CF.sub.3 H H CH.sub.2 COMe Ga CH.sub.2 CF.sub.3 H H CH.sub.2 COEt Ga CH.sub.2 CN H H H Ga CH.sub.2 CN H H Me Gb CH.sub.2 CN H H Et Gb CH.sub.2 CN H H Pr-n Gb CH.sub. 2 CN H H Pr-i Gb CH.sub.2 CN H H Bu-n Gc CH.sub.2 CN Me H H Ga CH.sub.2 CN Et H H Gb CH.sub.2 CN Me H Me Gb CH.sub.2 CN Me H Et Gb CH.sub.2 CN H Me Me Ga CH.sub.2 CN H Me Et Gb CH.sub.2 CN H H F Ga CH.sub.2 CN H H Cl Ga CH.sub.2 CN H H Br Gb CH.sub.2 CN H H I Gb CH.sub.2 CN H H CF.sub.3 Ga CH.sub.2 CN H H CH.sub.2 F Ga CH.sub.2 CN H H CH.sub.2 Cl Ga CH.sub.2 CN H H CH.sub.2 Br Gb CH.sub.2 CN H H CH.sub.2 I Gb CH.sub.2 CN H H CH.sub.2 CH.sub.2 F Ga CH.sub.2 CN H H CH.sub.2 CH.sub.2 Cl Ga CH.sub.2 CN H H CH.sub.2 CH.sub.2 Br Gb CH.sub.2 CN H H CH.sub.2 CH.sub.2 I Gb CH.sub.2 CN H H CH(CH.sub.3)CH.sub.2 F Ga CH.sub.2 CN H H CH(CH.sub.3)CH.sub.2 Cl Ga -CH.sub.2 CN H H CH(CH.sub.3 )CH.sub.2 Br Gb

CH.sub.2 CN H H CH(CH.sub.3)CH.sub.2 I Gb CH.sub.2 CN H H CH.sub.2 OMe Ga CH.sub.2 CN H H CH.sub.2 OEt Ga CH.sub.2 CN H H CH.sub.2 CH.sub.2 OMe Ga CH.sub.2 CN H H CH.sub.2 CH.sub.2 OEt Ga CH.sub.2 CN H H CH(CH.sub.3)CH.sub.2 OMe Gb CH.sub.2 CN H H CH(CH.sub.3)CH.sub.2 OEt Gb CH.sub.2 CN H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CN H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CN H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 CN H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CN H H CH.sub.2 SMe Ga CH.sub.2 CN H H CH.sub.2 SEt Ga CH.sub.2 CN H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CN H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 CN H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CN H H CH.sub.2 CN Ga CH.sub.2 CN H H CO.sub.2 Me Ga CH.sub. 2 CN H H CO.sub.2 Et Ga CH.sub.2 CN H H CO.sub.2 Pr-n Gb CH.sub.2 CN H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CN H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 CN H H CH.sub.2 CO.sub.2 Pr-n Gb CH.sub.2 CN H H COMe Ga CH.sub.2 CN H H COEt Ga CH.sub.2 CN H H COPr-n Gb CH.sub.2 CN H H CH.sub.2 COMe Ga CH.sub.2 CN H H CH.sub.2 COEt Ga CH.sub.2 CO.sub.2 Me H H H Ga CH.sub.2 CO.sub.2 Me H H Me Gb CH.sub.2 CO.sub.2 Me H H Et Gb CH.sub.2 CO.sub.2 Me H H Pr-n Gb CH.sub.2 CO.sub.2 Me H H Pr-i Gb CH.sub.2 CO.sub.2 Me H H Bu-n Gc CH.sub.2 CO.sub.2 Me Me H H Ga CH.sub.2 CO.sub.2 Me Et H H Gb CH.sub.2 CO.sub.2 Me Me H Me Gb CH.sub.2 CO.sub.2 Me Me H Et Gb CH.sub.2 CO.sub.2 Me H Me Me Ga CH.sub.2 CO.sub.2 Me H Me Et Gb CH.sub.2 CO.sub. 2 Me H H F Ga CH.sub.2 CO.sub.2 Me H H Cl Ga CH.sub.2 CO.sub.2 Me H H Br Gb CH.sub.2 CO.sub.2 Me H H I Gb CH.sub.2 CO.sub.2 Me H H CF.sub.3 Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 F Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 Cl Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 Br Gb CH.sub.2 CO.sub.2 Me

H H CH.sub.2 I Gb CH.sub.2 CO.sub.2 Me H H CH.sub.2 CH.sub.2 F Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 CH.sub.2 Cl Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 CH.sub.2 Br Gb CH.sub.2 CO.sub.2 Me H H CH.sub.2 CH.sub.2 I Gb CH.sub.2 CO.sub.2 Me H H CH(CH.sub.3)CH.sub.2 F Ga CH.sub.2 CO.sub.2 Me H H CH(CH.sub.3)CH.sub.2 Cl Ga CH.sub.2 CO.sub.2 Me H H CH(CH.sub.3)CH.sub.2 Br Gb CH.sub.2 CO.sub.2 Me H H CH(CH.sub.3)CH.sub.2 I Gb CH.sub.2 CO.sub.2 Me H H CH.sub.2 OMe Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 OEt Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 CH.sub.2 OMe Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 CH.sub.2 OEt Ga CH.sub.2 CO.sub.2 Me H H CH(CH.sub.3)CH.sub.2 OMe Gb CH.sub.2 CO.sub.2 Me H H CH(CH.sub.3)CH.sub.2 OEt Gb CH.sub.2 CO.sub.2 Me H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 SMe Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 SEt Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 CN Ga CH.sub.2 CO.sub.2 Me H H CO.sub.2 Me Ga CH.sub.2 CO.sub.2 Me H H CO.sub.2 Et Ga CH.sub.2 CO.sub.2 Me H H CO.sub.2 Pr-n Gb CH.sub.2 CO.sub.2 Me H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 CO.sub.2 Pr-n Gb CH.sub.2 CO.sub.2 Me H H COMe Ga CH.sub.2 CO.sub.2 Me H H COEt Ga CH.sub.2 CO.sub.2 Me H H COPr-n Gb CH.sub.2 CO.sub.2 Me H H CH.sub.2 COMe Ga CH.sub.2 CO.sub.2 Me H H CH.sub.2 COEt Ga CH.sub.2 CO.sub.2 Et H H H Ga CH.sub.2 CO.sub.2 Et H H Me Gb CH.sub.2 CO.sub.2 Et H H Et Gb CH.sub.2 CO.sub.2 Et Me H H Ga CH.sub.2 CO.sub.2 Et Et H H Gb CH.sub.2 CO.sub.2 Et Me H Me Gb CH.sub.2 CO.sub.2 Et Me H Et Gb CH.sub.2 CO.sub.2 Et H Me Me Ga CH.sub.2 CO.sub.2 Et H Me Et Gb CH.sub.2 CO.sub.2 Et H H CF.sub.3 Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 F Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 Cl Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 Br Gb CH.sub.2 CO.sub.2 Et H H CH.sub.2 I Gb CH.sub.2 CO.sub.2 Et H H CH.sub.2 OMe Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 OEt Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 SMe Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 SEt Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 CN Ga CH.sub.2 CO.sub.2 Et H H CO.sub.2 Me Ga CH.sub.2 CO.sub.2 Et H H CO.sub.2 Et Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 CO.sub.2 Et H H COMe Ga CH.sub.2 CO.sub.2 Et H H COEt Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 COMe Ga CH.sub.2 CO.sub.2 Et H H CH.sub.2 COEt Ga CH.sub.2 CO.sub.2 Pr-n H H H Ga CH.sub.2 CO.sub.2 Pr-n H H Me Gb CH.sub.2 CO.sub.2 Pr-n Me H H Ga CH.sub.2 CO.sub.2 Pr-n Me H Me Gb CH.sub.2 CO.sub.2 Pr-n H Me Me Ga CH.sub.2 CO.sub.2 Pr-n H H CF.sub.3 Ga CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 F Ga CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 Cl Ga CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 Br Gb CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 I Gb CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 OMe Ga CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 SMe Ga CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 CN Ga CH.sub.2 CO.sub.2 Pr-n H H CO.sub.2 Me Ga CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CO.sub.2 Pr-n H H COMe Ga CH.sub.2 CO.sub.2 Pr-n H H CH.sub.2 COMe Ga CH.sub.2 COMe H H H Ga CH.sub.2 COMe H H Me Gb CH.sub.2 COMe H H Et Gb CH.sub.2 COMe H H Pr-n Gb CH.sub.2 COMe H H Pr-i Gb CH.sub.2 COMe H H Bu-n Gc CH.sub.2 COMe Me H H Ga CH.sub.2 COMe Et H H Gb CH.sub.2 COMe Me H Me Gb CH.sub.2 COMe Me H Et Gb CH.sub.2 COMe H Me Me Ga CH.sub.2 COMe H Me Et Gb CH.sub.2 COMe H H F Ga CH.sub.2 COMe H H Cl Ga CH.sub.2 COMe H H Br Gb CH.sub.2 COMe H H I Gb

CH.sub.2 COMe H H CF.sub.3 Ga CH.sub.2 COMe H H CH.sub.2 F Ga CH.sub.2 COMe H H CH.sub.2 Cl Ga CH.sub.2 COMe H H CH.sub.2 Br Gb CH.sub.2 COMe H H CH.sub.2 I Gb CH.sub.2 COMe H H CH.sub.2 CH.sub.2 F Ga CH.sub.2 COMe H H CH.sub.2 CH.sub.2 Cl Ga CH.sub.2 COMe H H CH.sub.2 CH.sub.2 Br Gb CH.sub.2 COMe H H CH.sub.2 CH.sub.2 I Gb CH.sub.2 COMe H H CH(CH.sub.3)CH.sub.2 F Ga CH.sub.2 COMe H H CH(CH.sub.3)CH.sub.2 Cl Ga CH.sub.2 COMe H H CH(CH.sub.3)CH.sub.2 Br Gb CH.sub.2 COMe H H CH(CH.sub.3 )CH.sub.2 I Gb CH.sub.2 COMe H H CH.sub.2 OMe Ga CH.sub.2 COMe H H CH.sub.2 OEt Ga CH.sub.2 COMe H H CH.sub.2 CH.sub.2 OMe Ga CH.sub.2 COMe H H CH.sub.2 CH.sub.2 OEt Ga CH.sub.2 COMe H H CH(CH.sub.3)CH.sub.2 OMe Gb CH.sub.2 COMe H H CH(CH.sub.3)CH.sub.2 OEt Gb CH.sub.2 COMe H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 COMe H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 COMe H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 COMe H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 COMe H H CH.sub.2 SMe Ga CH.sub.2 COMe H H CH.sub.2 SEt Ga CH.sub.2 COMe H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 COMe H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 COMe H H CH.sub.2 CF.sub.3 Ga CH.sub.2 COMe H H CH.sub.2 CN Ga CH.sub.2 COMe H H CO.sub.2 Me Ga CH.sub.2 COMe H H CO.sub.2 Et Ga CH.sub.2 COMe H H CO.sub.2 Pr-n Gb CH.sub.2 COMe H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 COMe H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 COMe H H CH.sub.2 CO.sub.2 Pr-n Gb CH.sub.2 COMe H H COMe Ga CH.sub.2 COMe H H COEt Ga CH.sub.2 COMe H H COPr-n Gb CH.sub.2 COMe H H CH.sub.2 COMe Ga CH.sub.2 COMe H H CH.sub.2 COEt Ga CH.sub.2 COEt H H H Ga CH.sub.2 COEt H H Me Gb CH.sub.2 COEt H H Et Gb CH.sub.2 COEt Me H H Ga CH.sub.2 COEt Et H H Gb CH.sub.2 COEt Me H Me Gb CH.sub.2 COEt Me H Et Gb CH.sub.2 COEt H Me Me Ga CH.sub.2 COEt H Me Et Gb CH.sub.2 COEt H H CF.sub.3 Ga CH.sub.2 COEt H H CH.sub.2 F Ga CH.sub.2 COEt H H CH.sub.2 Cl Ga CH.sub.2 COEt H H CH.sub.2 Br Gb CH.sub.2 COEt H H CH.sub.2 I Gb CH.sub.2 COEt H H CH.sub.2 OMe Ga CH.sub.2 COEt H H CH.sub. 2 OEt Ga CH.sub.2 COEt H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 COEt H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 COEt H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 COEt H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 COEt H H CH.sub.2 SMe Ga CH.sub.2 COEt H H CH.sub.2 SEt Ga CH.sub.2 COEt H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 COEt H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 COEt H H CH.sub.2 CF.sub.3 Ga CH.sub.2 COEt H H CH.sub.2 CN Ga CH.sub.2 COEt H H CO.sub.2 Me Ga CH.sub.2 COEt H H CO.sub.2 Et Ga CH.sub.2 COEt H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 COEt H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 COEt H H COMe Ga CH.sub.2 COEt H H COEt Ga CH.sub.2 COEt H H CH.sub.2 COMe Ga CH.sub.2 COEt H H CH.sub.2 COEt Ga Ph H H H Ga Ph H H Me Ga PhCH.sub.2 H H H Gb PhCH.sub.2 H H Me Gb Me H H Ph Ga Me H H PhCH.sub.2 Gb Me H H CH.sub.2 CHCH.sub.2 Ga Me H H CH.sub.2 CCH Ga Bu-t H H H Gb ______________________________________

TABLE 8 __________________________________________________________________________ ##STR151## R.sup.21 R.sup.25 R.sup.26 R.sup.27 R.sup.28 Gn __________________________________________________________________________ H H H H H Ga H H H H Me Ga H H H H Et Ga H H H H Pr-n Gb H Me H H H Ga H H Me H H Ga H Me H H Me Gb H Me Me H Me Gb H H H Me Me Gb Me H H H H Ga Me H H H Me Ga Me H H H Et Ga Me H H H Pr-n Gb Me Me H H H Ga Me H Me H H Ga Me Me H H Me Gb Me Me Me H Me Gb Me H H Me Me Gb Me H H H CF.sub.3 Gb Me H H H CH.sub.2 F Gb Me H H H CH.sub.2 Cl Gb Me H H H CH.sub.2 Br Gb Me H H H CH.sub.2 I Gb Me H H H CH.sub.2 OMe Gb Me H H H CH.sub.2 OEt Gb Me H H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Gb Me H H H CH.sub.2 OCH.sub.2 CCH Gb Me H H H CH.sub.2 SMe Gb Me H H H CH.sub.2 SO.sub.2 Me Gb Me H H H CH.sub.2 CN Gb Me H H H CO.sub.2 Me Gb Me H H H CO.sub.2 Et Gb Me H H H COMe Gb Me H H H COEt Gb Me H H H CH.sub.2 CO.sub.2 Me Gb Me H H H CH.sub.2 CO.sub.2 Et Gb Me H H H CH.sub.2 COMe Gb Me H H H CH.sub.2 COEt Gb Et H H H H Ga Et H H H Me Ga Et H H H Et Ga Et H H H Pr-n Gb Et Me H H H Ga Et H Me H H Ga Et Me H H Me Gb Et Me Me H Me Gb Et H H Me Me Gb Et H H H CF.sub.3 Gb Et H H H CH.sub.2 F Gb Et H H H CH.sub.2 Cl Gb Et H H H CH.sub.2 Br Gb Et H H H CH.sub.2 I Gb Et H H H CH.sub.2 OMe Gb Et H H H CH.sub.2 OEt Gb Et H H H CH.sub.2 CN Gb Et H H H COMe Gb Et H H H COEt Gb Et H H H CH.sub.2 CO.sub.2 Me Gb Et H H H CH.sub.2 CO.sub.2 Et Gb Et H H H CH.sub.2 COMe Gb Et H H H CH.sub.2 COEt Gb Pr-n H H H H Ga Pr-n H H H Me Ga Pr-n H H H Et Ga Pr-n H H H Pr-n Gb Pr-n Me H H H Ga Pr-n H Me H H Ga Pr-n Me H H Me Gb Pr-n Me Me H Me Gb Pr-n H H Me Me Gb Pr-n H H H CF.sub.3 Gb Pr-n H H H CH.sub.2 F Gb Pr-n H H H CH.sub.2 Cl Gb Pr-n H H H CH.sub.2 Br Gb Pr-n H H H CH.sub.2 I Gb Pr-n H H H CH.sub.2 OMe Gb Pr-n H H H CH.sub.2 OEt Gb Pr-i H H H H Ga Pr-i H H H Me Ga Pr-i H H H Et Ga Pr-i H H H Pr-n Gb Pr-i Me H H H Ga Pr-i H Me H H Ga Pr-i Me H H Me Gb Pr-i Me Me H Me Gb Pr-i H H Me Me Gb Bu-n H H H H Ga Bu-n H H H Me Ga Bu-n H H H Et Ga Bu-n H H H Pr-n Gb CH.sub.2 CHCH.sub.2 H H H H Ga CH.sub.2 CHCH.sub.2 H H H Me Ga CH.sub.2 CHCH.sub.2 H H H Et Ga CH.sub.2 CHCH.sub.2 H H H Pr-n Gb CH.sub.2 CHCH.sub.2 Me H H H Ga CH.sub.2 CHCH.sub.2 H Me H H Ga CH.sub.2 CHCH.sub.2 Me H H Me Gb CH.sub.2 CHCH.sub.2 Me Me H Me Gb CH.sub.2 CHCH.sub.2 H H Me Me Gb CH.sub.2 CCH H H H H Ga CH.sub.2 CCH H H H Me Ga CH.sub.2 CCH H H H Et Ga CH.sub.2 CCH H H H Pr-n Gb CH.sub.2 CCH Me H H H Ga CH.sub.2 CCH H Me H H Ga CH.sub.2 CCH Me H H Me Gb CH.sub.2 CCH Me Me H Me Gb CH.sub.2 CCH H H Me Me Gb CH.sub.2 OMe H H H H Ga CH.sub.2 OMe H H H Me Ga CH.sub.2 OMe H H H Et Ga CH.sub.2 OMe H H H Pr-n Gb CH.sub.2 OMe Me H H H Ga CH.sub.2 OMe H Me H H Ga CH.sub.2 OMe Me H H Me Gb CH.sub.2 OMe Me Me H Me Gb CH.sub.2 OMe H H Me Me Gb CH.sub.2 OMe H H H CF.sub.3 Gb CH.sub.2 OMe H H H CH.sub.2 F Gb CH.sub.2 OMe H H H CH.sub.2 Cl Gb CH.sub.2 OMe H H H CH.sub.2 Br Gb CH.sub.2 OMe H H H CH.sub.2 I Gb CH.sub.2 OMe H H H CH.sub.2 OMe Gb CH.sub.2 OMe H H H CH.sub.2 OEt Gb CH.sub.2 OMe H H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Gb CH.sub.2 OMe H H H CH.sub.2 OCH.sub.2 CCH Gb CH.sub.2 OMe H H H CH.sub.2 SMe Gb CH.sub.2 OMe H H H CH.sub.2 SO.sub.2 Me Gb CH.sub.2 OMe H H H CH.sub.2 CN Gb CH.sub.2 OMe H H H CO.sub.2 Me Gb CH.sub.2 OMe H H H CO.sub.2 Et Gb CH.sub.2 OMe H H H COMe Gb CH.sub.2 OMe H H H COEt Gb CH.sub.2 OMe H H H CH.sub.2 CO.sub.2 Me Gb CH.sub.2 OMe H H H CH.sub.2 CO.sub.2 Et Gb CH.sub.2 OMe H H H CH.sub.2 COMe Gb CH.sub.2 OMe H H H CH.sub.2 COEt Gb CH.sub.2 OEt H H H H Ga CH.sub.2 OEt H H H Me Ga CH.sub.2 OEt H H H Et Ga CH.sub.2 OEt H H H Pr-n Gb CH.sub.2 OEt Me H H H Ga CH.sub.2 OEt H Me H H Ga CH.sub.2 OEt Me H H Me Gb CH.sub.2 OEt Me Me H Me Gb CH.sub.2 OEt H H Me Me Gb CH.sub.2 OEt H H H CF.sub.3 Gb CH.sub.2 OEt H H H CH.sub.2 F Gb CH.sub.2 OEt H H H CH.sub.2 Cl Gb CH.sub.2 OEt H H H CH.sub.2 Br Gb CH.sub.2 OEt H H H CH.sub.2 I Gb CH.sub.2 OEt H H H CH.sub.2 OMe Gb CH.sub.2 OEt H H H CH.sub.2 OEt Gb CH.sub.2 OEt H H H CH.sub.2 CN Gb CH.sub.2 OEt

H H H COMe Gb CH.sub.2 OEt H H H COEt Gb CH.sub.2 OEt H H H CH.sub.2 CO.sub.2 Me Gb CH.sub.2 OEt H H H CH.sub.2 CO.sub.2 Et Gb CH.sub.2 OEt H H H CH.sub.2 COMe Gb CH.sub.2 OEt H H H CH.sub.2 COEt Gb CH.sub.2 CH.sub.2 OMe H H H H Ga CH.sub.2 CH.sub.2 OMe H H H Me Ga CH.sub.2 CH.sub.2 OMe H H H Et Ga CH.sub.2 CH.sub.2 OMe H H H Pr-n Gb CH.sub.2 CH.sub.2 OMe Me H H H Ga CH.sub.2 CH.sub.2 OMe H Me H H Ga CH.sub.2 CH.sub.2 OMe Me H H Me Gb CH.sub.2 CH.sub.2 OMe Me Me H Me Gb CH.sub.2 CH.sub.2 OMe H H Me Me Gb CH.sub.2 CH.sub.2 OMe H H H CF.sub.3 Gb CH.sub.2 CH.sub.2 OMe H H H CH.sub.2 F Gb CH.sub.2 CH.sub.2 OMe H H H CH.sub.2 Cl Gb CH.sub.2 CH.sub.2 OMe H H H CH.sub.2 Br Gb CH.sub.2 CH.sub.2 OMe H H H CH.sub.2 I Gb CH.sub.2 CH.sub.2 OMe H H H CH.sub.2 OMe Gb CH.sub.2 CH.sub.2 OMe H H H CH.sub.2 OEt Gb CH.sub.2 CH.sub.2 OMe H H H CH.sub.2 CN Gb CH.sub.2 CH.sub.2 OMe H H H COMe Gb CH.sub.2 CH.sub.2 OMe H H H COEt Gb CH.sub.2 CH.sub.2 OMe H H H CH.sub.2 CO.sub.2 Me Gb CH.sub.2 CH.sub.2 OMe H H H CH.sub.2 CO.sub.2 Et Gb CH.sub.2 CH.sub.2 OMe H H H CH.sub.2 COMe Gb CH.sub.2 CH.sub.2 OMe H H H CH.sub.2 COEt Gb CH.sub.2 CH.sub.2 OEt H H H H Ga CH.sub.2 CH.sub.2 OEt H H H Me Ga CH.sub.2 CH.sub.2 OEt H H H Et Ga CH.sub.2 CH.sub.2 OEt H H H Pr-n Gb CH.sub.2 CH.sub.2 OEt Me H H H Ga CH.sub.2 CH.sub.2 OEt H Me H H Ga CH.sub.2 CH.sub.2 OEt Me H H Me Gb CH.sub.2 CH.sub.2 OEt Me Me H Me Gb CH.sub.2 CH.sub.2 OEt H H Me Me Gb CH.sub.2 CH.sub.2 OEt H H H CF.sub.3 Gb CH.sub.2 CH.sub.2 OEt H H H CH.sub.2 F Gb CH.sub.2 CH.sub.2 OEt H H H CH.sub.2 Cl Gb CH.sub.2 CH.sub.2 OEt H H H CH.sub.2 Br Gb CH.sub.2 CH.sub.2 OEt H H H CH.sub.2 I Gb CH.sub.2 CH.sub.2 OEt H H H CH.sub.2 OMe Gb CH.sub.2 CH.sub.2 OEt H H H CH.sub.2 OEt Gb CH(CH.sub.3)CH.sub.2 OMe H H H H Ga CH(CH.sub.3)CH.sub.2 OMe H H H Me Ga CH(CH.sub.3)CH.sub.2 OMe H H H Et Ga CH(CH.sub.3)CH.sub.2 OMe H H H Pr-n Gb CH(CH.sub.3)CH.sub.2 OMe Me H H H Ga CH(CH.sub.3)CH.sub.2 OMe H Me H H Ga CH(CH.sub.3)CH.sub.2 OMe Me H H Me Gb CH(CH.sub.3)CH.sub.2 OMe Me Me H Me Gb CH(CH.sub.3)CH.sub.2 OMe H H Me Me Gb CH(CH.sub.3)CH.sub.2 OMe H H H CF.sub.3 Gb CH(CH.sub.3)CH.sub.2 OMe H H H CH.sub.2 F Gb CH(CH.sub.3)CH.sub.2 OMe H H H CH.sub.2 Cl Gb CH(CH.sub.3)CH.sub.2 OMe H H H CH.sub.2 Br Gb CH(CH.sub.3)CH.sub.2 OMe H H H CH.sub.2 I Gb CH(CH.sub.3)CH.sub.2 OMe H H H CH.sub.2 OMe Gb CH(CH.sub.3)CH.sub.2 OMe H H H CH.sub.2 OEt Gb CH(CH.sub.3)CH.sub.2 OEt H H H H Ga CH(CH.sub.3)CH.sub.2 OEt H H H Me Ga CH(CH.sub.3)CH.sub.2 OEt H H H Et Ga CH(CH.sub.3)CH.sub.2 OEt H H H Pr-N Gb CH(CH.sub.3)CH.sub.2 OEt Me H H H Ga CH(CH.sub.3)CH.sub.2 OEt H Me H H Ga CH(CH.sub.3)CH.sub.2 OEt Me H H Me Gb CH(CH.sub.3)CH.sub.2 OEt Me Me H Me Gb CH(CH.sub.3)CH.sub.2 OEt H H Me Me Gb CH.sub.2 OCHF.sub.2 H H H H Ga CH.sub.2 OCHF.sub.2 H H H Me Ga CH.sub.2 OCHF.sub.2 H H H Et Ga CH.sub.2 OCHF.sub.2 H H H Pr-n Gb CH.sub.2 OCHF.sub.2 Me H H H Ga CH.sub.2 OCHF.sub.2 H Me H H Ga CH.sub.2 OCHF.sub.2 Me H H Me Gb CH.sub.2 OCHF.sub.2 Me Me H Me Gb CH.sub.2 OCHF.sub.2 H H Me Me Gb CH.sub.2 SMe H H H H Ga CH.sub.2 SMe H H H Me Ga CH.sub.2 SMe H H H Et Ga CH.sub.2 SMe H H H Pr-n Gb CH.sub.2 SMe Me H H H Ga CH.sub.2 SMe H Me H H Ga CH.sub.2 SMe Me H H Me Gb CH.sub.2 SMe Me Me H Me Gb CH.sub.2 SMe H H Me Me Gb CH.sub.2 SMe H H H CF.sub.3 Gb CH.sub.2 SMe H H H CH.sub.2 F Gb CH.sub.2 SMe H H H CH.sub.2 Cl Gb CH.sub.2 SMe H H H CH.sub.2 Br Gb CH.sub.2 SMe H H H CH.sub.2 I Gb CH.sub.2 SMe H H H CH.sub.2 OMe Gb CH.sub.2 SMe H H H CH.sub.2 OEt Gb CH.sub.2 SMe H H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Gb CH.sub.2 SMe H H H CH.sub.2 OCH.sub.2 CCH Gb CH.sub.2 SMe H H H CH.sub.2 SMe Gb CH.sub.2 SMe H H H CH.sub.2 SO.sub.2 Me Gb CH.sub.2 SMe H H H CH.sub.2 CN Gb CH.sub.2 SMe H H H CO.sub.2 Me Gb CH.sub.2 SMe H H H CO.sub.2 Et Gb CH.sub.2 SMe H H H COMe Gb CH.sub.2 SMe H H H COEt Gb CH.sub.2 SMe H H H CH.sub.2 CO.sub.2 Me Gb CH.sub.2 SMe H H H CH.sub.2 CO.sub.2 Et Gb CH.sub.2 SMe H H H CH.sub.2 COMe Gb CH.sub.2 SMe H H H CH.sub.2 COEt Gb CH.sub.2 SEt H H H H Ga CH.sub.2 SEt H H H Me Ga CH.sub.2 SEt H H H Et Ga CH.sub.2 SEt H H H Pr-n Gb CH.sub.2 SEt Me H H H Ga CH.sub.2 SEt H Me H H Ga CH.sub.2 SEt Me H H Me Gb CH.sub.2 SEt Me Me H Me Gb

CH.sub.2 SEt H H Me Me Gb CH.sub.2 SEt H H H CF.sub.3 Gb CH.sub.2 SEt H H H CH.sub.2 F Gb CH.sub.2 SEt H H H CH.sub.2 Cl Gb CH.sub.2 SEt H H H CH.sub.2 Br Gb CH.sub.2 SEt H H H CH.sub.2 I Gb CH.sub.2 SEt H H H CH.sub.2 OMe Gb CH.sub.2 SEt H H H CH.sub.2 OEt Gb CH.sub.2 SO.sub.2 Me H H H H Ga CH.sub.2 SO.sub.2 Me H H H Me Ga CH.sub.2 SO.sub.2 Me H H H Et Ga CH.sub.2 SO.sub.2 Me H H H Pr-n Gb CH.sub.2 SO.sub.2 Me Me H H H Ga CH.sub.2 SO.sub.2 Me H Me H H Ga CH.sub.2 SO.sub.2 Me Me H H Me Gb CH.sub.2 SO.sub.2 Me Me Me H Me Gb CH.sub.2 SO.sub.2 Me H H Me Me Gb CH.sub.2 SO.sub.2 Me H H H CF.sub.3 Gb CH.sub.2 SO.sub.2 Me H H H CH.sub.2 F Gb CH.sub.2 SO.sub.2 Me H H H CH.sub.2 Cl Gb CH.sub.2 SO.sub.2 Me H H H CH.sub.2 Br Gb CH.sub.2 SO.sub.2 Me H H H CH.sub.2 I Gb CH.sub.2 SO.sub.2 Me H H H CH.sub.2 OMe Gb CH.sub.2 SO.sub.2 Me H H H CH.sub.2 OEt Gb CH.sub.2 SO.sub.2 Et H H H H Ga CH.sub.2 SO.sub.2 Et H H H Me Ga CH.sub.2 SO.sub.2 Et H H H Et Ga CH.sub.2 SO.sub.2 Et H H H Pr-n Gb CH.sub.2 SO.sub.2 Et Me H H H Ga CH.sub.2 SO.sub.2 Et H Me H H Ga CH.sub.2 SO.sub.2 Et Me H H Me Gb CH.sub.2 SO.sub.2 Et Me Me H Me Gb CH.sub.2 SO.sub.2 Et H H Me Me Gb CH.sub.2 F H H H H Ga CH.sub.2 F H H H Me Ga CH.sub.2 F H H H Et Ga CH.sub.2 F H H H Pr-n Gb CH.sub.2 F Me H H H Ga CH.sub.2 F H Me H H Ga CH.sub.2 F Me H H Me Gb CH.sub.2 F Me Me H Me Gb CH.sub.2 F H H Me Me Gb CH.sub.2 F H H H CF.sub.3 Gb CH.sub.2 F H H H CH.sub.2 F Gb CH.sub.2 F H H H CH.sub.2 Cl Gb CH.sub.2 F H H H CH.sub.2 Br Gb CH.sub.2 F H H H CH.sub.2 I Gb CH.sub.2 F H H H CH.sub.2 OMe Gb CH.sub.2 F H H H CH.sub.2 OEt Gb CH.sub.2 Cl H H H H Ga CH.sub.2 Cl H H H Me Ga CH.sub.2 Cl H H H Et Ga CH.sub.2 Cl H H H Pr-n Gb CH.sub.2 Cl Me H H H Ga CH.sub.2 Cl H Me H H Ga CH.sub.2 Cl Me H H Me Gb CH.sub.2 Cl Me Me H Me Gb CH.sub.2 Cl H H Me Me Gb CH.sub.2 Cl H H H CF.sub.3 Gb CH.sub.2 Cl H H H CH.sub.2 F Gb CH.sub.2 Cl H H H CH.sub.2 Cl Gb CH.sub.2 Cl H H H CH.sub.2 Br Gb CH.sub.2 Cl H H H CH.sub.2 I Gb CH.sub.2 Cl H H H CH.sub.2 OMe Gb CH.sub.2 Cl H H H CH.sub.2 OEt Gb CH.sub.2 Br H H H H Ga CH.sub.2 Br H H H Me Ga CH.sub.2 Br H H H Et Ga CH.sub.2 Br H H H Pr-n Gb CH.sub.2 Br Me H H H Ga CH.sub.2 Br H Me H H Ga CH.sub.2 Br Me H H Me Gb CH.sub.2 Br Me Me H Me Gb CH.sub.2 Br H H Me Me Gb CH.sub.2 Br H H H CF.sub.3 Gb CH.sub.2 Br H H H CH.sub.2 F Gb CH.sub.2 Br H H H CH.sub.2 Cl Gb CH.sub.2 Br H H H CH.sub.2 Br Gb CH.sub.2 Br H H H CH.sub.2 I Gb CH.sub.2 Br H H H CH.sub.2 OMe Gb CH.sub.2 Br H H H CH.sub.2 OEt Gb CH.sub.2 I H H H H Ga CH.sub.2 I H H H Me Ga CH.sub.2 I H H H Et Ga CH.sub.2 I H H H Pr-n Gb CH.sub.2 I Me H H H Ga CH.sub.2 I H Me H H Ga CH.sub.2 I Me H H Me Gb CH.sub.2 I Me Me H Me Gb CH.sub.2 I H H Me Me Gb CH.sub.2 I H H H CF.sub.3 Gb CH.sub.2 I H H H CH.sub.2 F Gb CH.sub.2 I H H H CH.sub.2 Cl Gb CH.sub.2 I H H H CH.sub.2 Br Gb CH.sub.2 I H H H CH.sub.2 I Gb CH.sub.2 I H H H CH.sub.2 OMe Gb CH.sub.2 I H H H CH.sub.2 OEt Gb CH.sub.2 CH.sub.2 F H H H H Ga CH.sub.2 CH.sub.2 F H H H Me Ga CH.sub.2 CH.sub.2 F H H H Et Ga CH.sub.2 CH.sub.2 F H H H Pr-n Gb CH.sub.2 CH.sub.2 F Me H H H Ga CH.sub.2 CH.sub.2 F H Me H H Ga CH.sub.2 CH.sub.2 F Me H H Me Gb CH.sub.2 CH.sub.2 F Me Me H Me Gb CH.sub.2 CH.sub.2 F H H Me Me Gb CH.sub.2 CH.sub.2 Cl H H H H Ga CH.sub.2 CH.sub.2 Cl H H H Me Ga CH.sub.2 CH.sub.2 Cl H H H Et Ga CH.sub.2 CH.sub.2 Cl H H H Pr-n Gb CH.sub.2 CH.sub.2 Cl Me H H H Ga CH.sub.2 CH.sub.2 Cl H Me H H Ga CH.sub.2 CH.sub.2 Cl Me H H Me Gb CH.sub.2 CH.sub.2 Cl Me Me H Me Gb CH.sub.2 CH.sub.2 Cl H H Me Me Gb CH.sub.2 CH.sub.2 Br H H H H Ga CH.sub.2 CH.sub.2 Br H H H Me Ga CH.sub.2 CH.sub.2 Br H H H Et Ga CH.sub.2 CH.sub.2 Br H H H Pr-n Gb CH.sub.2 CH.sub.2 Br Me H H H Ga CH.sub.2 CH.sub.2 Br H Me H H Ga CH.sub.2 CH.sub.2 Br Me H H Me Gb CH.sub.2 CH.sub.2 Br Me Me H Me Gb CH.sub.2 CH.sub.2 Br H H Me Me Gb CH.sub.2 CH.sub.2 I H H H H Ga CH.sub.2 CH.sub.2 I H H H Me Ga CH.sub.2 CH.sub.2 I H H H Et Ga CH.sub.2 CH.sub.2 I H H H Pr-n Gb CH.sub.2 CH.sub.2 I Me H H H Ga CH.sub.2 CH.sub.2 I H Me H H Ga CH.sub.2 CH.sub.2 I Me H H Me Gb CH.sub.2 CH.sub.2 I Me Me H Me Gb CH.sub.2 CH.sub.2 I H H Me Me Gb CH(CH.sub.3)CH.sub.2 F H H H H Ga CH(CH.sub.3)CH.sub.2 F H H H Me Ga CH(CH.sub.3)CH.sub.2 F H H H Et Ga CH(CH.sub.3)CH.sub.2 F H H H Pr-n Gb CH(CH.sub.3)CH.sub.2 F

Me H H H Ga CH(CH.sub.3)CH.sub.2 F H Me H H Ga CH(CH.sub.3)CH.sub.2 F Me H H Me Gb CH(CH.sub.3)CH.sub.2 F Me Me H Me Gb CH(CH.sub.3)CH.sub.2 F H H Me Me Gb CH(CH.sub.3)CH.sub.2 Cl H H H H Ga CH(CH.sub.3)CH.sub.2 Cl H H H Me Ga CH(CH.sub.3)CH.sub.2 Cl H H H Et Ga CH(CH.sub.3)CH.sub.2 Cl H H H Pr-n Gb CH(CH.sub.3)CH.sub.2 Cl Me H H H Ga CH(CH.sub.3)CH.sub.2 Cl H Me H H Ga CH(CH.sub.3)CH.sub.2 Cl Me H H Me Gb CH(CH.sub.3)CH.sub.2 Cl Me Me H Me Gb CH(CH.sub.3)CH.sub.2 Cl H H Me Me Gb CH(CH.sub.3)CH.sub.2 Br H H H H Ga CH(CH.sub.3)CH.sub.2 Br H H H Me Ga CH(CH.sub.3)CH.sub.2 Br H H H Et Ga CH(CH.sub.3)CH.sub.2 Br H H H Pr-n Gb CH(CH.sub.3)CH.sub.2 Br Me H H H Ga CH(CH.sub.3)CH.sub.2 Br H Me H H Ga CH(CH.sub.3)CH.sub.2 Br Me H H Me Gb CH(CH.sub.3)CH.sub.2 Br Me Me H Me Gb CH(CH.sub.3)CH.sub.2 Br H H Me Me Gb CH(CH.sub.3)CH.sub.2 I H H H H Ga CH(CH.sub.3)CH.sub.2 I H H H Me Ga CH(CH.sub.3)CH.sub.2 I H H H Et Ga CH(CH.sub.3)CH.sub.2 I H H H Pr-n Gb CH(CH.sub.3)CH.sub.2 I Me H H H Ga CH(CH.sub.3)CH.sub.2 I H Me H H Ga CH(CH.sub.3)CH.sub.2 I Me H H Me Gb CH(CH.sub.3)CH.sub.2 I Me Me H Me Gb CH(CH.sub.3)CH.sub.2 I H H Me Me Gb CH.sub.2 CF.sub.3 H H H H Ga CH.sub.2 CF.sub.3 H H H Me Ga CH.sub.2 CF.sub.3 H H H Et Ga CH.sub.2 CF.sub.3 H H H Pr-n Gb CH.sub.2 CF.sub.3 Me H H H Ga CH.sub.2 CF.sub.3 H Me H H Ga

CH.sub.2 CF.sub.3 Me H H Me Gb CH.sub.2 CF.sub.3 Me Me H Me Gb CH.sub.2 CF.sub.3 H H Me Me Gb CH.sub.2 CF.sub.3 H H H CF.sub.3 Gb CH.sub.2 CF.sub.3 H H H CH.sub.2 F Gb CH.sub.2 CF.sub.3 H H H CH.sub.2 Cl Gb CH.sub.2 CF.sub.3 H H H CH.sub.2 Br Gb CH.sub.2 CF.sub.3 H H H CH.sub.2 I Gb CH.sub.2 CF.sub.3 H H H CH.sub.2 OMe Gb CH.sub.2 CF.sub.3 H H H CH.sub.2 OEt Gb CH.sub.2 CN H H H H Ga CH.sub.2 CN H H H Me Ga CH.sub.2 CN H H H Et Ga CH.sub.2 CN H H H Pr-n Gb CH.sub.2 CN Me H H H Ga CH.sub.2 CN H Me H H Ga CH.sub.2 CN Me H H Me Gb CH.sub.2 CN Me Me H Me Gb CH.sub.2 CN H H Me Me Gb CH.sub.2 CN H H H CF.sub.3 Gb CH.sub.2 CN H H H CH.sub.2 F Gb CH.sub.2 CN H H H CH.sub.2 Cl Gb CH.sub.2 CN H H H CH.sub.2 Br Gb CH.sub.2 CN H H H CH.sub.2 I Gb CH.sub.2 CN H H H CH.sub.2 OMe Gb CH.sub.2 CN H H H CH.sub.2 OEt Gb CH.sub.2 CO.sub.2 Me H H H H Ga CH.sub.2 CO.sub.2 Me H H H Me Ga CH.sub.2 CO.sub.2 Me H H H Et Ga CH.sub.2 CO.sub.2 Me H H H Pr-n Gb CH.sub.2 CO.sub.2 Me Me H H H Ga CH.sub.2 CO.sub.2 Me H Me H H Ga CH.sub.2 CO.sub.2 Me Me H H Me Gb CH.sub.2 CO.sub.2 Me Me Me H Me Gb CH.sub.2 CO.sub.2 Me H H Me Me Gb CH.sub.2 CO.sub.2 Me H H H CF.sub.3 Gb CH.sub.2 CO.sub.2 Me H H H CH.sub.2 F Gb CH.sub.2 CO.sub.2 Me H H H CH.sub.2 Cl Gb CH.sub.2 CO.sub.2 Me H H H CH.sub.2 Br Gb CH.sub.2 CO.sub.2 Me H H H CH.sub.2 I Gb CH.sub.2 CO.sub.2 Me H H H CH.sub.2 OMe Gb CH.sub.2 CO.sub.2 Me H H H CH.sub.2 OEt Gb CH.sub.2 CO.sub.2 Et H H H H Ga CH.sub.2 CO.sub.2 Et H H H Me Ga CH.sub.2 CO.sub.2 Et H H H Et Ga CH.sub.2 CO.sub.2 Et H H H Pr-n Gb CH.sub.2 CO.sub.2 Et Me H H H Ga CH.sub.2 CO.sub.2 Et H Me H H Ga CH.sub.2 CO.sub.2 Et Me H H Me Gb CH.sub.2 CO.sub.2 Et Me Me H Me Gb CH.sub.2 CO.sub.2 Et H H Me Me Gb CH.sub.2 CO.sub.2 Pr-n H H H H Ga CH.sub.2 CO.sub.2 Pr-n H H H Me Ga CH.sub.2 CO.sub.2 Pr-n H H H Et Ga CH.sub.2 CO.sub.2 Pr-n H H H Pr-n Gb CH.sub.2 CO.sub.2 Pr-n Me H H H Ga CH.sub.2 CO.sub.2 Pr-n H Me H H Ga CH.sub.2 CO.sub.2 Pr-n Me H H Me Gb CH.sub.2 CO.sub.2 Pr-n Me Me H Me Gb CH.sub.2 CO.sub.2 Pr-n H H Me Me Gb CH.sub.2 COMe H H H H Ga CH.sub.2 COMe H H H Me Ga CH.sub.2 COMe H H H Et Ga CH.sub.2 COMe H H H Pr-n Gb CH.sub.2 COMe Me H H H Ga CH.sub.2 COMe H Me H H Ga CH.sub.2 COMe Me H H Me Gb CH.sub.2 COMe Me Me H Me Gb CH.sub.2 COMe H H Me Me Gb CH.sub.2 COMe H H H CF.sub.3 Gb CH.sub.2 COMe H H H CH.sub.2 F Gb CH.sub.2 COMe H H H CH.sub.2 Cl Gb CH.sub.2 COMe H H H CH.sub.2 Br Gb CH.sub.2 COMe H H H CH.sub.2 I Gb CH.sub.2 COMe H H H CH.sub.2 OMe Gb CH.sub.2 COMe H H H CH.sub.2 OEt Gb CH.sub.2 COEt H H H H Ga CH.sub.2 COEt H H H Me Ga CH.sub.2 COEt H H H Et Ga CH.sub.2 COEt H H H Pr-n Gb CH.sub.2 COEt Me H H H Ga CH.sub.2 COEt H Me H H Ga CH.sub.2 COEt Me H H Me Gb CH.sub.2 COEt Me Me H Me Gb CH.sub.2 COEt H H Me Me Gb CH.sub.2 COEt H H H CF.sub.3 Gb CH.sub.2 COEt H H H CH.sub.2 F Gb CH.sub.2 COEt H H H CH.sub.2 Cl Gb CH.sub.2 COEt H H H CH.sub.2 Br Gb CH.sub. 2 COEt H H H CH.sub.2 I Gb CH.sub.2 COEt H H H CH.sub.2 OMe Gb CH.sub.2 COEt H H H CH.sub.2 OEt Gb Ph H H H H Ga PhCH.sub.2 H H H H Gb Ph H H H Me Ga PhCH.sub.2 H H H Me Gb Me H H H Ph Ga Me H H H PhCH.sub.2 Gb Me H H H Cl Gb Me H H H CH.sub.2CHCH.sub.2 Ga Me H H H CHCCH.sub.2 Ga __________________________________________________________________________

TABLE 9 ______________________________________ ##STR152## R.sup.21 R.sup.22 R.sup.23 R.sup.24 Gn ______________________________________ Me H H H Ga Me H H Me Ga Me H H Et Gb Me H H Pr-n Gb Me H H Pr-i Gb Me H H Bu-n Gc Me Me H H Ga Me Et H H Gb Me Me H Me Gb Me Me H Et Gb Me H Me Me Ga Me H Me Et Gb Me H H F Ga Me H H Cl Ga Me H H Br Gb Me H H I Gb Me H H CF.sub.3 Ga Me H H CH.sub.2 F Ga Me H H CH.sub.2 Cl Ga Me H H CH.sub.2 Br Gb Me H H CH.sub.2 I Gb Me H H CH.sub.2 CH.sub.2 F Ga Me H H CH.sub.2 CH.sub.2 Cl Ga Me H H CH.sub.2 CH.sub.2 Br Gb Me H H CH.sub.2 CH.sub.2 I Gb Me H H CH(CH.sub.3)CH.sub.2 F Ga Me H H CH(CH.sub.3)CH.sub.2 Cl Ga Me H H CH(CH.sub.3)CH.sub.2 Br Gb Me H H CH(CH.sub.3)CH.sub.2 I Gb Me H H CH.sub.2 OMe Ga Me H H CH.sub.2 OEt Ga Me H H CH.sub.2 CH.sub.2 OMe Ga Me H H CH.sub.2 CH.sub.2 OEt Ga Me H H CH(CH.sub.3)CH.sub.2 OMe Gb Me H H CH(CH.sub.3)CH.sub.2 OEt Gb Me H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga Me H H CH.sub.2 OCH.sub.2 CCH Ga Me H H CH.sub.2 OCHF.sub.2 Ga Me H H CH.sub.2 OCF.sub.3 Ga Me H H CH.sub.2 SMe Ga Me H H CH.sub.2 SEt Ga Me H H CH.sub.2 SO.sub.2 Me Ga Me H H CH.sub.2 SO.sub.2 Et Ga Me H H CH.sub.2 CF.sub.3 Ga Me H H CH.sub.2 CN Ga Me H H CO.sub.2 Me Ga Me H H CO.sub.2 Et Ga Me H H CO.sub.2 Pr-n Gb Me H H CH.sub.2 CO.sub.2 Me Ga Me H H CH.sub.2 CO.sub.2 Et Ga Me H H CH.sub.2 CO.sub.2 Pr-n Gb Me H H COMe Ga Me H H COEt Ga Me H H COPr-n Gb Me H H CH.sub.2 COMe Ga Me H H CH.sub.2 COEt Ga Et H H H Ga Et H H Me Ga Et H H Et Gb Et H H Pr-n Gb Et H H Pr-i Gb Et H H Bu-n Gc Et Me H H Ga Et Et H H Gb Et Me H Me Gb Et Me H Et Gb Et H Me Me Ga Et H Me Et Gb Et H H F Ga Et H H Cl Ga Et H H Br Gb Et H H I Gb Et H H CF.sub.3 Ga Et H H CH.sub.2 F Ga Et H H CH.sub.2 Cl Ga Et H H CH.sub.2 Br Gb Et H H CH.sub.2 I Gb Et H H CH.sub.2 CH.sub.2 F Ga Et H H CH.sub.2 CH.sub.2 Cl Ga Et H H CH.sub.2 CH.sub.2 Br Gb Et H H CH.sub.2 CH.sub.2 I Gb Et H H CH(CH.sub.3)CH.sub.2 F Ga Et H H CH(CH.sub.3)CH.sub.2 Cl Ga Et H H CH(CH.sub.3)CH.sub.2 Br Gb Et H H CH(CH.sub.3)CH.sub.2 I Gb Et H H CH.sub.2 OMe Ga Et H H CH.sub.2 OEt Ga Et H H CH.sub.2 CH.sub.2 OMe Ga Et H H CH.sub.2 CH.sub.2 OEt Ga Et H H CH(CH.sub.3)CH.sub.2 OMe Gb Et H H CH(CH.sub.3)CH.sub.2 OEt Gb Et H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga Et H H CH.sub.2 OCH.sub.2 CCH Ga Et H H CH.sub.2 OCHF.sub.2 Ga Et H H CH.sub.2 OCF.sub.3 Ga Et H H CH.sub.2 SMe Ga Et H H CH.sub.2 SEt Ga Et H H CH.sub.2 SO.sub.2 Me Ga Et H H CH.sub.2 SO.sub.2 Et Ga Et H H CH.sub.2 CF.sub.3 Ga Et H H CH.sub.2 CN Ga Et H H CO.sub.2 Me Ga Et H H CO.sub.2 Et Ga Et H H CO.sub.2 Pr-n Gb Et H H CH.sub.2 CO.sub.2 Me Ga Et H H CH.sub.2 CO.sub.2 Et Ga Et H H CH.sub.2 CO.sub.2 Pr-n Gb Et H H COMe Ga Et H H COEt Ga Et H H COPr-n Gb Et H H CH.sub.2 COMe Ga Et H H CH.sub.2 COEt Ga Pr-n H H H Ga Pr-n H H Me Gb Pr-n H H Et Gb Pr-n Me H H Ga Pr-n Et H H Gb Pr-n Me H Me Gb Pr-n Me H Et Gb Pr-n H Me Me Ga Pr-n H Me Et Gb Pr-n H H CF.sub.3 Ga Pr-n H H CH.sub.2 F Ga Pr-n H H CH.sub.2 Cl Ga Pr-n H H CH.sub.2 Br Gb Pr-n H H CH.sub.2 I Gb Pr-n H H CH.sub.2 OMe Ga Pr-n H H CH.sub.2 OEt Ga Pr-n H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga Pr-n H H CH.sub.2 OCH.sub.2 C CH Ga Pr-n H H CH.sub.2 OCHF.sub.2 Ga Pr-n H H CH.sub.2 OCF.sub.3 Ga Pr-n H H CH.sub.2 SMe Ga Pr-n H H CH.sub.2 SEt Ga Pr-n H H CH.sub.2 SO.sub.2 Me Ga Pr-n H H CH.sub.2 SO.sub.2 Et Ga Pr-n H H CH.sub.2 CF.sub.3 Ga Pr-n H H CH.sub.2 CN Ga Pr-n H H CO.sub.2 Me Ga Pr-n H H CO.sub.2 Et Ga Pr-n H H CH.sub.2 CO.sub.2 Me Ga Pr-n H H CH.sub.2 CO.sub.2 Et Ga Pr-n H H COMe Ga Pr-n H H COEt Ga Pr-n H H CH.sub.2 COMe Ga Pr-n H H CH.sub.2 COEt Ga Pr-i H H H Ga Pr-i H H Me Gb Pr-i H H Et Gb Pr-i Me H H Ga Pr-i Et H H Gb Pr-i Me H Me Gb Pr-i Me H Et Gb Pr-i H Me Me Ga Pr-i H Me Et Gb Pr-i H H CF.sub.3 Ga Pr-i H H CH.sub.2 F Ga Pr-i H H CH.sub.2 Cl Ga Pr-i H H CH.sub.2 Br Gb Pr-i H H CH.sub.2 I Gb Pr-i H H CH.sub.2 OMe Ga Pr-i H H CH.sub.2 OEt Ga Pr-i H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga Pr-i H H CH.sub.2 OCH.sub.2 CCH Ga Pr-i H H CH.sub.2 OCHF.sub.2 Ga Pr-i H H CH.sub.2 OCF.sub.3 Ga Pr-i H H CH.sub.2 SMe Ga Pr-i H H CH.sub.2 SEt Ga Pr-i H H CH.sub.2 SO.sub.2 Me Ga Pr-i H H CH.sub.2 SO.sub.2 Et Ga Pr-i H H CH.sub.2 CF.sub.3 Ga Pr-i H H CH.sub.2 CN Ga Pr-i H H CO.sub.2 Me Ga Pr-i H H CO.sub.2 Et Ga Pr-i H H CH.sub.2 CO.sub.2 Me Ga Pr-i H H CH.sub.2 CO.sub.2 Et Ga Pr-i H H COMe Ga Pr-i H H COEt Ga Pr-i H H CH.sub.2 COMe Ga Pr-i H H CH.sub.2 COEt Ga Bu-n H H H Ga Bu-n H H Me Gb Bu-n Me H H Ga Bu-n Me H Me Gb Bu-n H Me Me Ga Bu-n H H CF.sub.3 Ga Bu-n H H CH.sub.2 F Ga Bu-n H H CH.sub.2 Cl Ga

Bu-n H H CH.sub.2 Br Gb Bu-n H H CH.sub.2 I Gb Bu-n H H CH.sub.2 OMe Ga Bu-n H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga Bu-n H H CH.sub.2 OCH.sub.2 CCH Ga Bu-n H H CH.sub.2 OCHF.sub.2 Ga Bu-n H H CH.sub.2 OCF.sub.3 Ga Bu-n H H CH.sub.2 SMe Ga Bu-n H H CH.sub.2 SO.sub.2 Me Ga Bu-n H H CH.sub.2 CF.sub.3 Ga Bu-n H H CH.sub.2 CN Ga Bu-n H H CO.sub.2 Me Ga Bu-n H H CH.sub.2 CO.sub.2 Me Ga Bu-n H H COMe Ga Bu-n H H CH.sub.2 COMe Ga CH.sub.2 CHCH.sub.2 H H H Ga CH.sub.2 CHCH.sub.2 H H Me Gb CH.sub.2 CHCH.sub.2 H H Et Gb CH.sub.2 CHCH.sub.2 Me H H Ga CH.sub.2 CHCH.sub.2 Et H H Gb CH.sub.2 CHCH.sub.2 Me H Me Gb CH.sub.2 CHCH.sub.2 Me H Et Gb CH.sub.2 CHCH.sub.2 H Me Me Ga CH.sub.2 CHCH.sub.2 H Me Et Gb CH.sub.2 CHCH.sub.2 H H CF.sub.3 Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 F Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 Cl Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 Br Gb CH.sub.2 CHCH.sub.2 H H CH.sub.2 I Gb CH.sub.2 CHCH.sub.2 H H CH.sub.2 OMe Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 OEt Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 SMe Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 SEt Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 CN Ga CH.sub.2 CHCH.sub.2 H H CO.sub.2 Me Ga CH.sub.2 CHCH.sub.2 H H CO.sub.2 Et Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 CHCH.sub.2 H H COMe Ga CH.sub.2 CHCH.sub.2 H H COEt Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 COMe Ga CH.sub.2 CHCH.sub.2 H H CH.sub.2 COEt Ga CH.sub.2 CCH H H H Ga CH.sub.2 CCH H H Me Gb CH.sub.2 CCH H H Et Gb CH.sub.2 CCH Me H H Ga CH.sub.2 CCH Et H H Gb CH.sub.2 CCH Me H Me Gb CH.sub.2 CCH Me H Et Gb CH.sub.2 CCH H Me Me Ga CH.sub.2 CCH H H F Ga CH.sub.2 CCH H Me Et Gb CH.sub.2 CCH H H CF.sub.3 Ga CH.sub.2 CCH H H CH.sub.2 F Ga CH.sub.2 CCH H H CH.sub.2 Cl Ga CH.sub.2 CCH H H CH.sub.2 Br Gb CH.sub.2 CCH H H CH.sub.2 I Gb CH.sub.2 CCH H H CH.sub.2 OMe Ga CH.sub.2 CCH H H CH.sub.2 OEt Ga CH.sub.2 CCH H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga CH.sub.2 CCH H H CH.sub.2 OCH.sub.2 CCH Ga CH.sub.2 CCH H H CH.sub.2 OCHF.sub.2 Ga CH.sub.2 CCH H H CH.sub.2 OCF.sub.3 Ga CH.sub.2 CCH H H CH.sub.2 SMe Ga CH.sub.2 CCH H H CH.sub.2 SEt Ga CH.sub.2 CCH H H CH.sub.2 SO.sub.2 Me Ga CH.sub.2 CCH H H CH.sub.2 SO.sub.2 Et Ga CH.sub.2 C CH H H CH.sub.2 CF.sub.3 Ga CH.sub.2 CCH H H CH.sub.2 CN Ga CH.sub.2 CCH H H CO.sub.2 Me Ga CH.sub.2 CCH H H CO.sub.2 Et Ga CH.sub.2 CCH H H CH.sub.2 CO.sub.2 Me Ga CH.sub.2 CCH H H CH.sub.2 CO.sub.2 Et Ga CH.sub.2 CCH H H COMe Ga CH.sub.2 CCH H H COEt Ga CH.sub.2 CCH H H CH.sub.2 COMe Ga CH.sub.2 CCH H H CH.sub.2 COEt Ga ______________________________________

TABLE 10 ______________________________________ ##STR153## R.sup.21 R.sup.25 R.sup.26 R.sup.27 R.sup.28 Gn ______________________________________ Me H H H H Ga Me H H H Me Ga Me H H H Et Ga Me H H H Pr-n Gb Me Me H H H Ga Me H Me H H Ga Me Me H H Me Gb Me Me Me H Me Gb Me H H Me Me Gb Me H H H CF.sub.3 Gb Me H H H CH.sub.2 F Gb Me H H H CH.sub.2 Cl Gb Me H H H CH.sub.2 Br Gb Me H H H CH.sub.2 I Gb Me H H H CH.sub.2 OMe Gb Me H H H CH.sub.2 OEt Gb Me H H H CH.sub.2 OCH.sub.2 CHCH.sub.2 Gb Me H H H CH.sub.2 OCH.sub.2 CCH Gb Me H H H CH.sub.2 SMe Gb Me H H H CH.sub.2 SO.sub.2 Me Gb Me H H H CH.sub.2 CN Gb Me H H H CO.sub.2 Me Gb Me H H H CO.sub.2 Et Gb Me H H H COMe Gb Me H H H COEt Gb Me H H H CH.sub.2 CO.sub.2 Me Gb Me H H H CH.sub.2 CO.sub.2 Et Gb Me H H H CH.sub.2 COMe Gb Me H H H CH.sub.2 COEt Gb Et H H H H Ga Et H H H Me Ga Et H H H Et Ga Et H H H Pr-n Gb Et Me H H H Ga Et H Me H H Ga Et Me H H Me Gb Et Me Me H Me Gb Et H H Me Me Gb Et H H H CF.sub.3 Gb Et H H H CH.sub.2 F Gb Et H H H CH.sub.2 Cl Gb Et H H H CH.sub.2 Br Gb Et H H H CH.sub.2 I Gb Et H H H CH.sub.2 OMe Gb Et H H H CH.sub.2 OEt Gb Et H H H CH.sub.2 CN Gb Et H H H COMe Gb Et H H H COEt Gb Et H H H CH.sub.2 CO.sub.2 Me Gb Et H H H CH.sub.2 CO.sub.2 Et Gb Et H H H CH.sub.2 COMe Gb Et H H H CH.sub.2 COEt Gb Pr-n H H H H Ga Pr-n H H H Me Ga Pr-n H H H Et Ga Pr-n H H H Pr-n Gb Pr-n Me H H H Ga Pr-n H Me H H Ga Pr-n Me H H Me Gb Pr-n Me Me H Me Gb Pr-n H H Me Me Gb Pr-n H H H CF.sub.3 Gb Pr-n H H H CH.sub.2 F Gb Pr-n H H H CH.sub.2 Cl Gb Pr-n H H H CH.sub.2 Br Gb Pr-n H H H CH.sub.2 I Gb Pr-n H H H CH.sub.2 OMe Gb Pr-n H H H CH.sub.2 OEt Gb Pr-i H H H H Ga Pr-i H H H Me Ga Pr-i H H H Et Ga Pr-i H H H Pr-n Gb Pr-i Me H H H Ga Pr-i H Me H H Ga Pr-i Me H H Me Gb Pr-i Me Me H Me Gb Pr-i H H Me Me Gb Bu-n H H H H Ga Bu-n H H H Me Ga Bu-n H H H Et Ga Bu-n H H H Pr-n Gb CH.sub.2 CHCH.sub.2 H H H H Ga CH.sub.2 CHCH.sub.2 H H H Me Ga CH.sub.2 CHCH.sub.2 H H H Et Ga CH.sub.2 CHCH.sub.2 H H H Pr-n Gb CH.sub.2 CHCH.sub.2 Me H H H Ga CH.sub.2 CHCH.sub.2 H Me H H Ga CH.sub.2 CHCH.sub.2 Me H H Me Gb CH.sub.2 CHCH.sub.2 Me Me H Me Gb CH.sub.2 CHCH.sub.2 H H Me Me Gb CH.sub.2 CCH H H H H Ga CH.sub.2 CCH H H H Me Ga CH.sub.2 CCH H H H Et Ga CH.sub.2 CCH H H H Pr-n Gb CH.sub.2 CCH Me H H H Ga CH.sub.2 CCH H Me H H Ga CH.sub.2 CCH Me H H Me Gb CH.sub.2 CCH Me Me H Me Gb CH.sub.2 CCH H H Me Me Gb ______________________________________

TABLE 11 ______________________________________ ##STR154## R.sup.21 R.sup.22 R.sup.23 R.sup.24 Gn ______________________________________ Me H H H Gc Me H H Me Gc Me H H Et Gc Me Me H H Gc Me Et H H Gc Me Me H Me Gc Me H Me Me Gc Et H H H Gc Et H H Me Gc Et H H Et Gc Et Me H H Gc Et H Me Me Gc ______________________________________

TABLE 12 ______________________________________ ##STR155## R.sup.21 R.sup.25 R.sup.26 R.sup.27 R.sup.28 Gn ______________________________________ Me H H H H Gc Me H H H Me Gc Me H H H Et Gc Me Me H H H Gc Me H Me H H Gc Me H H Me Me Gc Me Me H H Me Gc Et H H H H Gc Et H H Me Me Gc Et Me H H H Gc Et H H H Me Gc ______________________________________

TABLE 13 ______________________________________ ##STR156## R.sup.21 R.sup.22 R.sup.23 R.sup.24 Gn ______________________________________ Me H H H Gc Me H H Me Gc Me H H Et Gc Me Me H H Gc Me Et H H Gc Me Me H Me Gc Me H Me Me Gc Et H H H Gc Et H H Me Gc Et H H Et Gc Et Me H H Gc Et H Me Me Gc ______________________________________

TABLE 14 ______________________________________ ##STR157## R.sup.21 R.sup.25 R.sup.26 R.sup.27 R.sup.28 Gn ______________________________________ Me H H H H Gc Me H H H Me Gc Me H H H Et Gc Me Me H H H Gc Me H Me H H Gc Me H H Me Me Gc Me Me H H Me Gc Et H H H H Gc Et H H H Me Gc Et Me H H H Gc Et H H Me Me Gc ______________________________________

TABLE 1A ______________________________________ ##STR158## R.sup.11 R.sup.12 R.sup.13 Gn ______________________________________ Me Me Me G.sub.1 Me Me Me G.sub.3 Me Me Me G.sub.5 Me Me Me G.sub.6 Me Me Me G.sub.7 Me Me Me G.sub.8 Me Me Me G.sub.11 Me Me Me G.sub.12 Me Me Me G.sub.13 Me Me Me G.sub.14 Me Me Me G.sub.15 Me Me Me G.sub.16 Me Me Me G.sub.19 Me Me Me G.sub.20 Me Me Me G.sub.23 Me Me Me G.sub.25 Me Me Me G.sub.26 Me Me Me G.sub.27 Me Me Me G.sub.29 Me Me Me G.sub.31 Me Me Me G.sub.34 Me Me Me G.sub.36 Me Me Me G.sub.39 Me Me Me G.sub.41 Me Me Me G.sub.42 Me Me Me G.sub.44 Me Me Me G.sub.99 Me Me Me G.sub.100 Me Me Me G.sub.103 Me Me Me G.sub.116 Me Me Me G.sub. 117 Me Me Me G.sub.120 Me Me Me G.sub.121 Me Me Me G.sub.122 Me Me Me G.sub.123 Me Me Me G.sub.124 Me Me Me G.sub.125 Me Me Me G.sub.126 Me Me Me G.sub.129 Me Me Me G.sub.132 Me Me Me G.sub.144 Me Me Me G.sub.180 Me Me Me G.sub.181 Me Me Me G.sub.189 Me Me Me G.sub.190 Me Me Me G.sub.192 Me Me Me G.sub.193 Me Me Me G.sub.194 Me Me Me G.sub.196 Me Me Me G.sub.197 Me Me Me G.sub.198 Me Me Me G.sub.209 Me Me Me G.sub.213 Me Me Me G.sub.214 Me Me Me G.sub.215 Me Me Me G.sub.219 Me Me Me G.sub.220 Me Me Me G.sub.221 Me Me Me G.sub.222 Me Me Me G.sub.224 Me Me Me G.sub.226 Me Me Me G.sub.229 Me Me Me G.sub.232 Me Me Me G.sub.235 Me Me Me G.sub.236 Me Me Me G.sub.238 Me Me Me G.sub.248 Me Me Me G.sub.250 Me Me Me G.sub.259 Me Me Me G.sub.262 Me Me Me G.sub. 265 Me Me Me G.sub.267 Me Me Me G.sub.268 Me Me Me G.sub.269 Me Me Me G.sub.270 Me Me Me G.sub.271 Me Me Me G.sub.272 Me Me Me G.sub.273 Me Me Me G.sub.274 Me Me Me G.sub.275 Me Me Me G.sub.276 Me Me Me G.sub.277 Me Me Me G.sub.278 Me Me Me G.sub.280 Me Me Me G.sub.283 Me Me Me G.sub.286 Me Me Me G.sub.289 Me Me Me G.sub.292 Me Me Me G.sub.295 Me Me Me G.sub.296 Me Me Me G.sub.298 Me Me Me G.sub.299 Me Me Me G.sub.301 Me Me Me G.sub.302 Me Me Me G.sub.304 Me Me Me G.sub.305 Me Me Me G.sub.309 Me Me Me G.sub.310 Me Me Me G.sub.311 Me Me Me G.sub.316 Me Me Me G.sub.317 Me Me Me G.sub.319 Me Me Me G.sub.320 Me Me Me G.sub.328 Me Me Me G.sub.329 Me Me Me G.sub.334 Me Me Me G.sub.335 Me Me Me G.sub.343 Me Me Me G.sub.344 Me Me Me G.sub.346 Me Me Me G.sub. 347 Me Me Me G.sub.349 Me Me Me G.sub.350 Me Me Me G.sub.352 Me Me Me G.sub.353 Me Me Me G.sub.355 Me Me Me G.sub.356 Me Me Me G.sub.358 Me Me Me G.sub.359 Me Me Me G.sub.364 Me Me Me G.sub.367 Me Me Me G.sub.370 Me Me Me G.sub.373 Me Me Me G.sub.376 Me Me Me G.sub.377 Me Me Me G.sub.382 Me Me Me G.sub.383 Me Me Me G.sub.385 Me Me Me G.sub.386 Me Me Me G.sub.394 Me Me Me G.sub.395 Me Me Me G.sub.403 Me Me Me G.sub.406 Me Me Me G.sub.409 Me Me Me G.sub.415 Me Me Me G.sub.421 Me Me Me G.sub.427 Me Me Me G.sub.430 Me Me Me G.sub.439 Me Me Me G.sub.448 Me Me Me G.sub.451 Me Me Me G.sub.454 Me Me Me G.sub.455 Me Me Me G.sub.457 Me Me Me G.sub.458 Me Me Me G.sub.463 Me Me Me G.sub.464 Me Me Me G.sub.469 Me Me Me G.sub.472 Me Me Me G.sub.475 Me Me Me G.sub. 478 Me Me Me G.sub.484 Me Me Me G.sub.498 Me Me Me G.sub.499 Me Me Me G.sub.500 Me Me Me G.sub.501 Me Me Me G.sub.503 Me Me Me G.sub.504 Me Me Me G.sub.505 Me Me Me G.sub.506 Me Me Me G.sub.507 Me Me Me G.sub.508 Me Me Me G.sub.509 Me Me Me G.sub.510 Me Me Me G.sub.511 Me Me Me G.sub.512 Me Me Me G.sub.513 Me Me Me G.sub.514 Me Me Me G.sub.515 Me Me Me G.sub.537 Me Me Me G.sub.538 Me Me Me G.sub.539 Me Me Me G.sub.543 Me Me Me G.sub.544 Me Me Me G.sub.545 Me Me Me G.sub.549 Me Me Me G.sub.550 Me Me Me G.sub.551 Me Me Me G.sub.555 Me Me Me G.sub.556 Me Me Me G.sub.557 Me Me Me G.sub.561 Me Me Me G.sub.562 Me Me Me G.sub.563 Me Me Me G.sub.567 Me Me Me G.sub.568 Me Me Me G.sub.569 Me Me Me G.sub.573 Me Me Me G.sub.574 Me Me Me G.sub.575 Me Me Me G.sub. 579 Me Me Me G.sub.580 Me Me Me G.sub.581 Me Me Me G.sub.585 Me Me Me G.sub.586 Me Me Me G.sub.587 Me Me Me G.sub.593 Me Me Me G.sub.598 Me Me Me G.sub.599 Me Me Me G.sub.601 Me Me Me G.sub.606 Me Me Me G.sub.608 Me Me Me G.sub.610 Me Me Me G.sub.611 Me Me Me G.sub.612 Me Me Me G.sub.613 Me Me Me G.sub.614 Me Me Me G.sub.615 Me Me Me G.sub.617 Me Me Me G.sub.618 Me Me Me G.sub.620 Me Me Me G.sub.621 Me Me Me G.sub.622 Me Me Me G.sub.626 Me Me Me G.sub.627 Me Me Me G.sub.628 Me Me Me G.sub.632 Me Me Me G.sub.633 Me Me Me G.sub.634 Me Me Me G.sub.638 Me Me Me G.sub.639 Me Me Me G.sub.640 Me Me Me G.sub.643 Me Me Et G.sub.3 Me Me Et G.sub.6 Me Me Et G.sub.268 Me Me Et G.sub.269 Me Me Et G.sub.271 Me Me Et G.sub.272 Me Me Et G.sub.274 Me Me Et G.sub. 275 Me Me Et G.sub.277 Me Me Et G.sub.278 Me Me Et G.sub.355 Me Me Ph G.sub.3 Me Me Ph G.sub.6 Me Et Et G.sub.3 Me Et Et G.sub.6 Me (CH.sub.2).sub.4 G.sub.3 Me (CH.sub.2).sub.4 G.sub.6 Me (CH.sub.2).sub.5 G.sub.3 Me (CH.sub.2).sub.5

G.sub.6 Et Me Me G.sub.3 Et Me Me G.sub.6 Et Me Me G.sub.268 Et Me Me G.sub.269 Et Me Me G.sub.271 Et Me Me G.sub.272 Et Me Me G.sub.274 Et Me Me G.sub.275 Et Me Me G.sub.277 Et Me Me G.sub.278 Et Me Me G.sub.355 Et Me Et G.sub.3 Et Me Et G.sub.6 Et Me Ph G.sub.3 Et Me Ph G.sub.6 Et Et Et G.sub.3 Et Et Et G.sub.6 Et (CH.sub.2).sub.4 G.sub.3 Et (CH.sub.2).sub.4 G.sub.6 Et (CH.sub.2).sub.5 G.sub.3 Et (CH.sub.2).sub.5 G.sub.6 Pr-n Me Me G.sub.3 Pr-n Me Me G.sub.6 Pr-i Me Me G.sub.3 Pr-i Me Me G.sub.6 cyc-Pr Me Me G.sub.3 cyc-Pr Me Me G.sub.6 cyc-Pr Me Me G.sub.268 cyc-Pr Me Me G.sub.269 cyc-Pr Me Me G.sub.271 cyc-Pr Me Me G.sub.272 cyc-Pr Me Me G.sub.274 cyc-Pr Me Me G.sub.275 cyc-Pr Me Me G.sub.277 cyc-Pr Me Me G.sub.278 cyc-Pr Me Me G.sub.355 cyc-PrCH.sub.2 Me Me G.sub.3 cyc-PrCH.sub.2 Me Me G.sub.6 Bu-n Me Me G.sub.3 Bu-n Me Me G.sub.6 Bu-sec Me Me G.sub.3 Bu-sec Me Me G.sub.6 Bu-i Me Me G.sub.3 Bu-i Me Me G.sub.6 cyc-Bu Me Me G.sub.3 cyc-Bu Me Me G.sub.6 Bu-t Me Me G.sub.3 Bu-t Me Me G.sub.6 CH.sub.2CHCH.sub.2 Me Me G.sub.3 CH.sub.2CHCH.sub.2 Me Me G.sub.6 CHCCH.sub.2 Me Me G.sub.3 CHCCH.sub.2 Me Me G.sub.6 cyc-Pen Me Me G.sub.3 cyc-Pen Me Me G.sub.6 cyc-Hex Me Me G.sub.3 cyc-Hex Me Me G.sub.6 MeOCH.sub.2 CH.sub.2 Me Me G.sub.3 MeOCH.sub.2 CH.sub.2 Me Me G.sub.6 MeOCH.sub.2 (CH.sub.3)CH Me Me G.sub.3 MeOCH.sub.2 (CH.sub.3)CH Me Me G.sub.6 CHF.sub.2 OCH.sub.2 Me Me G.sub.3 CHF.sub.2 OCH.sub.2 Me Me G.sub.6 FCH.sub.2 Me Me G.sub.3 FCH.sub.2 Me Me G.sub.6 FCH.sub.2 CH.sub.2 Me Me G.sub.3 FCH.sub.2 CH.sub.2 Me Me G.sub.6 ClCH.sub.2 CH.sub.2 Me Me G.sub.3 ClCH.sub.2 CH.sub.2 Me Me G.sub.6 CF.sub.3 CH.sub.2 Me Me G.sub.3 CF.sub.3 CH.sub.2 Me Me G.sub.6 NCCH.sub.2 Me Me G.sub.3 NCCH.sub.2 Me Me G.sub.6 MeO.sub.2 CCH.sub.2 Me Me G.sub.3 MeO.sub.2 CCH.sub.2 Me Me G.sub.6 MeO.sub.2 CCH.sub.2 Me Me G.sub.268 MeO.sub.2 CCH.sub.2 Me Me G.sub.269 MeO.sub.2 CCH.sub.2 Me Me G.sub.271 MeO.sub.2 CCH.sub.2 Me Me G.sub.272 MeO.sub.2 CCH.sub.2 Me Me G.sub.274 MeO.sub.2 CCH.sub.2 Me Me G.sub.275 MeO.sub.2 CCH.sub.2 Me Me G.sub.277 MeO.sub.2 CCH.sub.2 Me Me G.sub.278 MeO.sub.2 CCH.sub.2 Me Me G.sub.355 MeCOCH.sub.2 Me Me G.sub.3 MeCOCH.sub.2 Me Me G.sub.6 PhCH.sub.2 Me Me G.sub.3 PhCH.sub.2 Me Me G.sub.6 Ph Me Me G.sub.3 Ph Me Me G.sub.6 Ph Me Me G.sub.268 Ph Me Me G.sub.269 Ph Me Me G.sub.271 Ph Me Me G.sub.272 Ph Me Me G.sub.274 Ph Me Me G.sub.275 Ph Me Me G.sub.277 Ph Me Me G.sub.278 Ph Me Me G.sub.355 Ph-2-Me Me Me G.sub.3 Ph-2-Me Me Me G.sub.6 Ph-3-Me Me Me G.sub.3 Ph-3-Me Me Me G.sub.6 Ph-4-OMe Me Me G.sub.3 Ph-4-OMe Me Me G.sub.6 Ph-3-OMe Me Me G.sub.3 Ph-3-OMe Me Me G.sub.6 Ph-2-OMe Me Me G.sub.3 Ph-2-OMe Me Me G.sub.6 Ph-4-Cl Me Me G.sub.3 Ph-4-Cl Me Me G.sub.6 Ph-3-Cl Me Me G.sub.3 Ph-3-Cl Me Me G.sub.6 Ph-2-Cl Me Me G.sub.3 Ph-2-Cl Me Me G.sub.6 Ph-2,6-Cl.sub.2 Me Me G.sub.3 Ph-2,6-Cl.sub.2 Me Me G.sub.6 ______________________________________

TABLE 2A ______________________________________ ##STR159## R.sup.11 R.sup.12 R.sup.13 Gn ______________________________________ Me Me Me G.sub.3 Me Me Me G.sub.6 Me Me Me G.sub.268 Me Me Me G.sub.269 Me Me Me G.sub.271 Me Me Me G.sub.272 Me Me Me G.sub.274 Me Me Me G.sub.275 Me Me Me G.sub.277 Me Me Me G.sub.278 Me Me Me G.sub.355 Me Me Et G.sub.3 Me Me Et G.sub.6 Me Me Ph G.sub.3 Me Me Ph G.sub.6 Et Me Me G.sub.3 Et Me Me G.sub.6 Et Me Me G.sub.268 Et Me Me G.sub.269 Et Me Me G.sub.271 Et Me Me G.sub.272 Et Me Me G.sub.274 Et Me Me G.sub.275 Et Me Me G.sub.277 Et Me Me G.sub.278 Et Me Me G.sub.355 Pr-n Me Me G.sub.3 Pr-n Me Me G.sub.6 Pr-i Me Me G.sub.3 Pr-i Me Me G.sub.6 CH.sub.2CHCH.sub.2 Me Me G.sub.3 CH.sub.2CHCH.sub.2 Me Me G.sub.6 CHCCH.sub.2 Me Me G.sub.3 CHCCH.sub.2 Me Me G.sub.6 MeOCH.sub.2 Me Me G.sub.3 MeOCH.sub.2 Me Me G.sub.6 MeSCH.sub.2 Me Me G.sub.3 MeSCH.sub.2 Me Me G.sub.6 MeO.sub.2 CCH.sub.2 Me Me G.sub.3 MeO.sub.2 CCH.sub.2 Me Me G.sub.6 Ph Me Me G.sub.3 Ph Me Me G.sub.6 PhCH.sub.2 Me Me G.sub.3 PhCH.sub.2 Me Me G.sub.6 ______________________________________

TABLE 3A ______________________________________ ##STR160## R.sup.11 R.sup.12 R.sup.13 Gn ______________________________________ Me Me Me G.sub.3 Me Me Me G.sub.6 Me Me Me G.sub.268 Me Me Me G.sub.269 Me Me Me G.sub.271 Me Me Me G.sub.272 Me Me Me G.sub.274 Me Me Me G.sub.275 Me Me Me G.sub.277 Me Me Me G.sub.278 Me Me Me G.sub.355 Et Me Me G.sub.3 Et Me Me G.sub.6 Pr-n Me Me G.sub.3 Pr-n Me Me G.sub.6 cyc-Pr Me Me G.sub.3 cyc-Pr Me Me G.sub.6 Me Me Et G.sub.3 Me Me Et G.sub.6 Me Et Me G.sub.3 Me Et Me G.sub.6 Me (CH.sub.2).sub.3 G.sub.3 Me (CH.sub.2).sub.3 G.sub.6 Me (CH.sub.2).sub.4 G.sub.3 Me (CH.sub.2).sub.4 G.sub.6 ______________________________________

TABLE 4A ______________________________________ ##STR161## R.sup.11 R.sup.12 R.sup.13 Gn ______________________________________ Me Me Me G.sub.3 Me Me Me G.sub.6 Me Me Et G.sub.3 Me Me Et G.sub.6 Et Me Me G.sub.3 Et Me Me G.sub.6 Pr-n Me Me G.sub.3 Pr-n Me Me G.sub.6 CH.sub.2CHCH.sub.2 Me Me G.sub.3 CH.sub.2CHCH.sub.2 Me Me G.sub.6 CHCCH.sub.2 Me Me G.sub.3 CHCCH.sub.2 Me Me G.sub.6 ______________________________________

TABLE 5A ______________________________________ ##STR162## R.sup.11 R.sup.12 R.sup.13 Gn ______________________________________ Me Me Me G.sub.3 Me Me Me G.sub.6 Me Me Et G.sub.3 Me Me Et G.sub.6 Et Me Me G.sub.3 Et Me Me G.sub.6 Pr-n Me Me G.sub.3 Pr-n Me Me G.sub.6 CH.sub.2CHCH.sub.2 Me Me G.sub.3 CH.sub.2CHCH.sub.2 Me Me G.sub.6 ______________________________________

TABLE 6A ______________________________________ ##STR163## R.sup.11 R.sup.12 R.sup.13 Gn ______________________________________ Me Me Me G.sub.3 Me Me Me G.sub.6 Et Me Me G.sub.3 Et Me Me G.sub.6 cyc-Pr Me Me G.sub.3 cyc-Pr Me Me G.sub.6 CH.sub.2CHCH.sub.2 Me Me G.sub.3 CH.sub.2CHCH.sub.2 Me Me G.sub.6 CHCCH.sub.2 Me Me G.sub.3 CHCCH.sub.2 Me Me G.sub.6 Me Me Et G.sub.3 Me Me Et G.sub.6 Me Et Me G.sub.3 Me Et Me G.sub.6 ______________________________________

TABLE 7A ______________________________________ ##STR164## R.sup.21 R.sup.22 R.sup.23 R.sup.24 Gn ______________________________________ H H H H G.sub.3 H H H H G.sub.6 Me H H H G.sub.3 Me H H H G.sub.6 Me H H H G.sub.268 Me H H H G.sub.269 Me H H H G.sub.271 Me H H H G.sub.272 Me H H H G.sub.274 Me H H H G.sub.275 Me H H H G.sub.277 Me H H H G.sub.278 Me H H H G.sub.355 Me H H Me G.sub.3 Me H H Me G.sub.6 Me H H Me G.sub.268 Me H H Me G.sub.269 Me H H Me G.sub.271 Me H H Me G.sub.272 Me H H Me G.sub.274 Me H H Me G.sub.275 Me H H Me G.sub.277 Me H H Me G.sub.278 Me H H Me G.sub.355 Me H H Et G.sub.3 Me H H Et G.sub.6 Me H Me Me G.sub.3 Me H Me Me G.sub.6 Et H H H G.sub.3 Et H H H G.sub.6 Et H H H G.sub.268 Et H H H G.sub.269 Et H H H G.sub.271 Et H H H G.sub.272 Et H H H G.sub.274 Et H H H G.sub.275 Et H H H G.sub.277 Et H H H G.sub.278 Et H H H G.sub.355 Pr-n H H H G.sub.3 Pr-n H H H G.sub.6 Pr-i H H H G.sub.3 Pr-i H H H G.sub.6 Bu-n H H H G.sub.3 Bu-n H H H G.sub.6 Bu-t H H H G.sub.3 Bu-t H H H G.sub.6 CH.sub.2CHCH.sub.2 H H H G.sub.3 CH.sub.2CHCH.sub.2 H H H G.sub.6 CHCCH.sub.2 H H H G.sub.3 CH CCH.sub.2 H H H G.sub.6 MeOCH.sub.2 H H H G.sub.3 MeOCH.sub.2 H H H G.sub.6 MeO.sub.2 CCH.sub.2 H H H G.sub.3 MeO.sub.2 CCH.sub.2 H H H G.sub.6 ______________________________________

TABLE 8A ______________________________________ ##STR165## R.sup.21 R.sup.25 R.sup.26 R.sup.27 R.sup.28 Gn ______________________________________ Me H H H H G.sub.1 Me H H H H G.sub.3 Me H H H H G.sub.5 Me H H H H G.sub.6 Me H H H H G.sub.7 Me H H H H G.sub.8 Me H H H H G.sub.11 Me H H H H G.sub.12 Me H H H H G.sub.13 Me H H H H G.sub.14 Me H H H H G.sub.15 Me H H H H G.sub.16 Me H H H H G.sub.19 Me H H H H G.sub.20 Me H H H H G.sub.23 Me H H H H G.sub.25 Me H H H H G.sub.26 Me H H H H G.sub.27 Me H H H H G.sub.29 Me H H H H G.sub.31 Me H H H H G.sub.34 Me H H H H G.sub.36 Me H H H H G.sub.39 Me H H H H G.sub.41 Me H H H H G.sub.42 Me H H H H G.sub.44 Me H H H H G.sub.99 Me H H H H G.sub.100 Me H H H H G.sub.103 Me H H H H G.sub.116 Me H H H H G.sub.117 Me H H H H G.sub.120 Me H H H H G.sub.121 Me H H H H G.sub.122 Me H H H H G.sub.123 Me H H H H G.sub.124 Me H H H H G.sub.125 Me H H H H G.sub.126 Me H H H H G.sub.129 Me H H H H G.sub.132 Me H H H H G.sub.144 Me H H H H G.sub.180 Me H H H H G.sub.181 Me H H H H G.sub.189 Me H H H H G.sub.190 Me H H H H G.sub.192 Me H H H H G.sub. 193 Me H H H H G.sub.194 Me H H H H G.sub.196 Me H H H H G.sub.197 Me H H H H G.sub.198 Me H H H H G.sub.209 Me H H H H G.sub.213 Me H H H H G.sub.214 Me H H H H G.sub.215 Me H H H H G.sub.219 Me H H H H G.sub.220 Me H H H H G.sub.221 Me H H H H G.sub.222 Me H H H H G.sub.224 Me H H H H G.sub.226 Me H H H H G.sub.229 Me H H H H G.sub.232 Me H H H H G.sub.235 Me H H H H G.sub.236 Me H H H H G.sub.238 Me H H H H G.sub.248 Me H H H H G.sub.250 Me H H H H G.sub.259 Me H H H H G.sub.262 Me H H H H G.sub.265 Me H H H H G.sub.267 Me H H H H C.sub.268 Me H H H H C.sub.269 Me H H H H G.sub.270 Me H H H H G.sub.271 Me H H H H G.sub.272 Me H H H H G.sub.273 Me H H H H G.sub.274 Me H H H H G.sub.275 Me H H H H G.sub.276 Me H H H H G.sub.277 Me H H H H G.sub.278 Me H H H H G.sub.280 Me H H H H G.sub.283 Me H H H H G.sub.286 Me H H H H G.sub.289 Me H H H H G.sub.292 Me H H H H G.sub.295 Me H H H H G.sub.296 Me H H H H G.sub.298 Me H H H H G.sub.299 Me H H H H G.sub.301 Me H H H H G.sub.302 Me H H H H G.sub.304 Me H H H H G.sub.305 Me H H H H G.sub.309 Me H H H H G.sub.310 Me H H H H G.sub.311 Me H H H H G.sub.316 Me H H H H G.sub.317 Me H H H H G.sub.320 Me H H H H G.sub.328 Me H H H H G.sub.329 Me H H H H G.sub.334 Me H H H H G.sub.335 Me H H H H G.sub.343 Me H H H H G.sub.344 Me H H H H G.sub.346 Me H H H H G.sub.347 Me H H H H G.sub.349 Me H H H H G.sub.350 Me H H H H G.sub.352 Me H H H H G.sub.353 Me H H H H G.sub.355 Me H H H H G.sub.356 Me H H H H G.sub.358 Me H H H H G.sub.359 Me H H H H G.sub.364 Me H H H H G.sub.367 Me H H H H G.sub.370 Me H H H H G.sub.373 Me H H H H G.sub.376 Me H H H H G.sub.377 Me H H H H G.sub.382 Me H H H H G.sub.383 Me H H H H G.sub.385 Me H H H H G.sub.386 Me H H H H G.sub.394 Me H H H H G.sub.395 Me H H H H G.sub.403 Me H H H H G.sub.406 Me H H H H G.sub.409 Me H H H H G.sub.415 Me H H H H G.sub.421 Me H H H H G.sub.427 Me H H H H G.sub.430 Me H H H H G.sub.439 Me H H H H G.sub.448 Me H H H H G.sub.451 Me H H H H G.sub.454 Me H H H H G.sub.455 Me H H H H G.sub.457 Me H H H H G.sub.458 Me H H H H G.sub.463 Me H H H H G.sub.464 Me H H H H G.sub.469 Me H H H H G.sub.472 Me H H H H G.sub.475 Me H H H H G.sub.478 Me H H H H G.sub.484 Me H H H H G.sub.498 Me H H H H G.sub.499 Me H H H H G.sub.500 Me H H H H G.sub.501 Me H H H H G.sub.503 Me H H H H G.sub.504 Me H H H H G.sub.505 Me H H H H G.sub.506 Me H H H H G.sub.507 Me H H H H G.sub.508 Me H H H H G.sub.509 Me H H H H G.sub.510 Me H H H H G.sub.511 Me H H H H G.sub.512 Me H H H H G.sub.513 Me H H H H G.sub.514 Me H H H H G.sub.515 Me H H H H G.sub.537 Me H H H H G.sub.538 Me H H H H G.sub.539 Me H H H H G.sub.543 Me H H H H G.sub.544 Me H H H H G.sub.545 Me H H H H G.sub.549 Me H H H H G.sub.550 Me H H H H G.sub.551 Me H H H H G.sub.555 Me H H H H G.sub.556 Me H H H H G.sub.557 Me H H H H G.sub.561 Me H H H H G.sub.562 Me H H H H G.sub.563 Me H H H H G.sub.567 Me H H H H G.sub.568 Me H H H H G.sub.569 Me H H H H G.sub.573 Me H H H H G.sub.574 Me H H H H G.sub.575 Me H H H H G.sub.579 Me H H H H G.sub.580 Me H H H H G.sub.581 Me H H H H G.sub.585 Me H H H H G.sub.586 Me H H H H G.sub.587 Me H H H H G.sub.593 Me H H H H G.sub.598 Me H H H H G.sub.599 Me H H H H G.sub.601 Me H H H H G.sub.606 Me H H H H G.sub.608 Me H H H H G.sub.610 Me H H H H G.sub.611 Me H H H H G.sub.612 Me H H H H G.sub.613 Me H H H H G.sub.614 Me H H H H G.sub.615 Me H H H H G.sub.617 Me H H H H G.sub.618 Me H H H H G.sub.620 Me H H H H G.sub.621 Me H H H H G.sub.622 Me H H H H G.sub.626 Me H H H H G.sub.627 Me H H H H G.sub.628 Me H H H H G.sub.632 Me H H H H G.sub.633 Me H H H H G.sub.634 Me H H H H G.sub.638 Me H H H H G.sub.639 Me H H H H G.sub.640 Me H H H H G.sub.643 Me H H H Me G.sub.3 Me H H H Me G.sub.6 Me H H H Me G.sub.268 Me H H H Me G.sub.269 Me H H H Me G.sub.271 Me H H H Me G.sub.272 Me H H H Me G.sub.274 Me H H H Me G.sub.275 Me H H H Me G.sub.277 Me H H H Me G.sub.278 Me H H H Me G.sub.355 Me Me H H H G.sub.3 Me Me H H H G.sub.6 Et H H H H G.sub.3 Et H H H H G.sub.6 Et H H H H G.sub.268 Et H H H H G.sub.269 Et H H H H G.sub.271 Et H H H H G.sub.272 Et H H H H G.sub.274 Et H H H H G.sub.275 Et H H H H G.sub.277 Et H H H H G.sub.278 Et H H H H G.sub. 355

Pr-n H H H H G.sub.3 Pr-n H H H H G.sub.6 CH.sub.2CHCH.sub.2 H H H H G.sub.3 CH.sub.2CHCH.sub.2 H H H H G.sub.6 CH CCH.sub.2 H H H H G.sub.3 CH CCH.sub.2 H H H H G.sub.6 ______________________________________

TABLE 9A ______________________________________ ##STR166## R.sup.21 R.sup.22 R.sup.23 R.sup.24 Gn ______________________________________ Me H H H G.sub.3 Me H H H G.sub.6 Me H H H G.sub.268 Me H H H G.sub.269 Me H H H G.sub.271 Me H H H G.sub.272 Me H H H G.sub.274 Me H H H G.sub.275 Me H H H G.sub.277 Me H H H G.sub.278 Me H H H G.sub.355 Me H H Me G.sub.3 Me H H Me G.sub.6 Et H H H G.sub.3 Et H H H G.sub.6 CH.sub.2CHCH.sub.2 H H H G.sub.3 CH.sub.2CHCH.sub.2 H H H G.sub.6 CHCCH.sub.2 H H H G.sub.3 CHCCH.sub.2 H H H G.sub.6 ______________________________________

TABLE 10A ______________________________________ ##STR167## R.sup.21 R.sup.25 R.sup.26 R.sup.27 R.sup.28 Gn ______________________________________ Me H H H H G.sub.3 Me H H H H G.sub.6 Me H H H H G.sub.268 Me H H H H G.sub.269 Me H H H H G.sub.271 Me H H H H G.sub.272 Me H H H H G.sub.274 Me H H H H G.sub.275 Me H H H H G.sub.277 Me H H H H G.sub.278 Me H H H H G.sub.355 Et H H H H G.sub.3 Et H H H H G.sub.6 CH.sub.2CHCH.sub.2 H H H H G.sub.3 CH.sub.2CHCH.sub.2 H H H H G.sub.6 CH CCH.sub.2 H H H H G.sub.3 CHCCH.sub.2 H H H H G.sub.6 ______________________________________

TABLE 11A ______________________________________ ##STR168## R.sup.21 R.sup.22 R.sup.23 R.sup.24 Gn ______________________________________ Me H H H G.sub.3 Me H H H G.sub.6 Me H H Me G.sub.3 Me H H Me G.sub.6 ______________________________________

TABLE 12A ______________________________________ ##STR169## R.sup.21 R.sup.25 R.sup.26 R.sup.27 R.sup.28 Gn ______________________________________ Me H H H H G.sub.3 Me H H H H G.sub.6 Et H H H H G.sub.3 Et H H H H G.sub.6 ______________________________________

TABLE 13A ______________________________________ ##STR170## R.sup.21 R.sup.22 R.sup.23 R.sup.24 Gn ______________________________________ Me H H H G.sub.3 Me H H H G.sub.6 Me H H Me G.sub.3 Me H H Me G.sub.6 ______________________________________

TABLE 14A ______________________________________ ##STR171## R.sup.21 R.sup.25 R.sup.26 R.sup.27 R.sup.28 Gn ______________________________________ Me H H H H G.sub.3 Me H H H H G.sub.6 Et H H H H G.sub.3 Et H H H H G.sub.6 ______________________________________


The compound of the present invention can be applied to control various weeds not only in the agricultural and horticultural fields such as upland fields, paddy fields or orchards, but also in non-agricultural fields such as play grounds, non-used vacant fields or railway sides.

The dose varies depending upon the application site, the season for application, the manner of application, the type of weeds to be controlled, the type of crop plants, etc. However, the dose is usually within a range of from 0.0001 to 10 kg per hectare, preferably from 0.005 to 5 kg per hectare, as the amount of the active ingredient.

Further, the compound of the present invention may be combined with other herbicides, various insecticides, fungicides, plant growth regulating agents and synergism agents at the time of the preparation of the formulations or at the time of the application, as the case requires.

Particularly, by the combined application with other herbicide, it can be expected to reduce the cost due to a decrease of the dose or to enlarge the herbicidal spectrum or obtain higher herbicidal effects due to a synergistic effect of the combined herbicides. In such a case, the compound of the present invention may be combined with a plurality of known herbicides. The herbicides of the type which can be used in combination with the compound of the present invention, may, for example, be compounds disclosed in Farm Chemicals Handbook (1990).

When the compound of the present invention is to be used as a herbicide, it is usually mixed with a suitable carrier, for instance, a solid carrier such as clay, talc, bentonite, diatomaceous earth or fine silica powder, or a liquid carrier such as water, an alcohol (such as isopropanol, butanol, benzyl alcohol or furfuryl alcohol), an aromatic hydrocarbon (such as toluene or xylene), an ether (such as anisole), a ketone (such as cyclohexanone or isophorone), an ester (such as butyl acetate), an acid amide (such as N-methylpyrrolidone), or a halogenated hydrocarbon (such as chlorobenzene). If desired, a surfactant, an emulsifier, a dispersing agent, a penetrating agent, a spreader, a thickener, an antifreezing agent, a coagulation preventing agent or a stabilizer may be added to prepare an optional formulation such as a liquid formulation, an emulsifiable concentrate, a wettable powder, a dry flowable, a flowable, a dust or a granule.

Now, Formulation Examples of the herbicides containing the compounds of the present invention as active ingredients, will be given. However, it should be understood that the present invention is by no means restricted to such specific Examples. In the following Formulation Examples, "parts" means "parts by weight".

    ______________________________________
    Wettable powder
    ______________________________________
    Compound of the present invention
                         5-80 parts
    Solid carrier        10-85 parts
    Surfactant           1-10 parts
    Other                1-5 parts
    ______________________________________


As other, a coagulation preventing agent may, for example, be mentioned.

    ______________________________________
    Emulsifiable concentrate
    Compound of the present invention
                         1-30 parts
    Liquid carrier       30-95 parts
    Surfactant           5-15 parts
    Flowable
    Compound of the present invention
                         5-70 parts
    Liquid carrier       15-65 parts
    Surfactant           5-12 parts
    Other                5-30 parts
    ______________________________________


As other, an antifreezing agent and a thickener may, for example, be mentioned.

    ______________________________________
    Granular wettable powder (dry flowable)
    Compound of the present invention
                            20-90 parts
    Solid carrier           10-60 parts
    Surfactant              1-20 parts
     Granule
    Compound of the present invention
                            0.1-10 parts
    Solid carrier           90-99.99 parts
    Other                   1-5 parts
    ______________________________________


FORMULATION EXAMPLE 1

Wettable powder

    ______________________________________
    Compound No. 2 of the present invention
                             20 parts
    Zeeklite A (tradename for a kaolin-type
                             76 parts
    clay, manufactured by Zeeklite Industries,
    Co., Ltd.)
    Sorpol 5039 (tradename for a mixture of a
                             2 parts
    nonionic surfactant and an anionic
    surfactant, manufactured by Toho Chemical
    Industry Co., Ltd.)
    Carplex (tradename for a coagulation-
                             2 parts
    preventing agent composed of a mixture of a
    surfactant and fine silica powder,
    manufactured by Shionogi Pharmaceutical
    Co., Ltd.)
    ______________________________________


The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

FORMULATION EXAMPLE 2

Wettable powder

    ______________________________________
    Compound No. 3 of the present invention
                             40 parts
    Zeeklite A (tradename for a kaolin-type
                             54 parts
    clay, manufactured by Zeeklite Industries,
    Co., Ltd.)
    Sorpol 5039 (tradename for a mixture of a
                             2 parts
    nonionic surfactant and an anionic
    surfactant, manufactured by Toho Chemical
    Industry Co., Ltd.)
    Carplex (tradename for a coagulation-
                             4 parts
    preventing agent composed of a mixture of a
    surfactant and fine silica powder,
    manufactured by Shionogi Pharmaceutical
    Co., Ltd.)
    ______________________________________


The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

FORMULATION EXAMPLE 3

Emulsifiable concentrate

    ______________________________________
    Compound No. 5 of the present invention
                             5 parts
    Xylene                   75 parts
    N,N-dimethylformamide    15 parts
    Sorpol 2680 (tradename for a mixture of a
                             5 parts
    nonionic surfactant and an anionic
    surfactant, manufactured by Toho Chemical
    Industry Co., Ltd.)
    ______________________________________


The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

FORMULATION EXAMPLE 4

Flowable

    ______________________________________
    Compound No. 6 of the present invention
                               25     parts
    Agrizole S-710 (tradename for a nonionic
                               10     parts
    surfactant, manufactured by Kao Corp.)
    Runox 1000C (tradename for an anionic
                               0.5    part
    surfactant, manufactured by Toho Chemical
    Industry Co., Ltd.)
    1% Rodopol water (tradename for a thickener,
                               20     parts
    manufactured by Rhone-Poulenc)
    Water                      44.5   parts
    ______________________________________


The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE 5

Flowable

    ______________________________________
    Compound No. 11 of the present invention
                               40     parts
    Agrizole S-710 (tradename for a nonionic
                               10     parts
    surfactant, manufactured by Kao Corp.)
    Runox 1000C (tradename for an anionic
                               0.5    part
    surfactant, manufactured by Toho Chemical
    Industry Co., Ltd.)
    1% Rodopol water (tradename for a thickener,
                               20     parts
    manufactured by Rhone-Poulenc)
    Water                      29.5   parts
    ______________________________________


The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE 6

Granular wettable powder (dry flowable)

    ______________________________________
    Compound No. 12 of the present invention
                               75     parts
    Isoban No. 1 (tradename for an anionic
                               10     parts
    surfactant, manufactured by Kuraray Isoprene
    Chemical Co., Ltd.)
    Vanirex N (tradename for an anionic
                               5      parts
    surfactant, manufactured by Sanyo Kokusaku
    Pulp Co., Ltd.)
    Carplex #80 (tradename for fine silica powder,
                               10     parts
    manufactured by Shionogi Pharmaceutical
    Co., Ltd.)
    ______________________________________


The above ingredients are uniformly mixed and pulverized to form a dry flowable.

FORMULATION EXAMPLE 7

Granule

    ______________________________________
    Compound No. 13 of the present invention
                            1      part
    Bentonite               55     parts
    Talc                    44     parts
    ______________________________________


The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

FORMULATION EXAMPLE 8

Wettable powder

    ______________________________________
    Compound No. 14 of the present invention
                             20 parts
    Zeeklite A (tradename for a kaolin-type
                             76 parts
    clay, manufactured by Zeeklite Industries,
    Co., Ltd.)
    Sorpol 5039 (tradename for a mixture of a
                             2 parts
    nonionic surfactant and an anionic
    surfactant, manufactured by Toho Chemical
    Industry Co., Ltd.)
    Carplex (tradename for a coagulation-
                             2 parts
    preventing agent composed of a mixture of a
    surfactant and fine silica powder,
    manufactured by Shionogi Pharmaceutical
    Co., Ltd.)
    ______________________________________


The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

FORMULATION EXAMPLE 9

Wettable powder

    ______________________________________
    Compound No. 15 of the present invention
                            40 parts
    Zeeklite A (tradename for a kaolin-type
                            54 parts
    clay, manufactured by Zeeklite Industries,
    Co., Ltd.)
    Sorpol 5039 (tradename for a mixture of a
                            2 parts
    nonionic surfactant and an anionic
    surfactant, manufactured by Toho Chemical
    Industry Co., Ltd.)
    Carplex (tradename for a coagulation-
                            4 parts
    preventing agent composed of a mixture of a
    surfactant and fine silica powder,
    manufactured by Shionogi Pharmaceutical
    Co., Ltd.)
    ______________________________________


The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

FORMULATION EXAMPLE 10

Emulsifiable concentrate

    ______________________________________
    Compound No. 31 of the present invention
                             5 parts
    Xylene                   75 parts
    N,N-dimethylformamide    15 parts
    Sorpol 2680 (tradename for a mixture of a
                             5 parts
    nonionic surfactant and an anionic
    surfactant, manufactured by Toho Chemical
    Industry Co., Ltd.)
    ______________________________________


The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

FORMULATION EXAMPLE 11

Flowable

    ______________________________________
    Compound No. 35 of the present invention
                               25     parts
    Agrizole S-710 (tradename for a nonionic
                               10     parts
    surfactant, manufactured by Kao Corp.)
    Runox 1000C (tradename for an anionic
                               0.5    part
    surfactant, manufactured by Toho Chemical
    Industry Co., Ltd.)
    1% Rodopol water (tradename for a thickener,
                               20     parts
    manufactured by Rhone-Poulenc)
    Water                      44.5   parts
    ______________________________________


The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE 12

Flowable

    ______________________________________
    Compound No. 42 of the present invention
                               40     parts
    Agrizole S-710 (tradename for a nonionic
                               10     parts
    surfactant, manufactured by Kao Corp.)
    Runox 1000C (tradename for an anionic
                               0.5    part
    surfactant, manufactured by Toho Chemical
    Industry Co., Ltd.)
    1% Rodopol water (tradename for a thickener,
                               20     parts
    manufactured by Rhone-Poulenc)
    Water                      44.5   parts
    ______________________________________


The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE 13

Granular wettable powder (dry flowable)

    ______________________________________
    Compound No. 47 of the present invention
                               75 parts
    Isoban No. 1 (tradename for an anionic
                               10 parts
    surfactant, manufactured by Kuraray Isoprene
    Chemical Co., Ltd.)
    Vanirex N (tradename for an anionic
                               5 parts
    surfactnt, manufactured by Sanyo Kokusaku
    Pulp Co., Ltd.)
    Carplex #80 (tradename for fine silica powder,
                               10 parts
    manufactured by Shionogi Pharmaceutical
    Co., Ltd.)
    ______________________________________


The above ingredients are uniformly mixed and pulverized to form a dry flowable.

FORMULATION EXAMPLE 14

Granule

    ______________________________________
    Compound No. 53 of the present invention
                             1      part
    Bentonite                55     parts
    Talc                     44     parts
    ______________________________________


The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

In use, the above wettable powder, emulsifiable concentrate, flowable or granular wettable powder is diluted with water from 50 to 1,000 times and applied so that the active ingredient will be from 0.0001 to 10 kg per hectare.

Now, the herbicidal activities of the compounds of the present invention will be described in detail with reference to the following Test Examples.

TEST EXAMPLE 1

Test on the herbicidal effects in soil treatment

A plastic box having a length of 15 cm, a width of 22 cm and a depth of 6 cm was filled with a sterilized diluvial soil, and seeds of Echinochloa crus-galli, Digitaria adscendens, Cyperus microiria, Solanum nigrum, Galinsoga ciliata, Rorippa indica, orvza sativa, Zea mays, Triticum aestivum, Glycine max and Gossypium herbaceum were sown, and the soil was covered thereon, and then a herbicide solution was applied by a small spray onto the surface of the soil uniformly so that the active ingredient was distributed at a predetermined concentration. The herbicide solution was prepared by diluting the formulation as described in the foregoing Formulation Examples with water and applied onto the entire soil surface. Three weeks after the application of the herbicidal solution, the herbicidal effects against each weed and the phytotoxicities against each crop plant were determined on the basis of the following standard ratings. The results are shown in Table 15.

Standard ratinqs:

5: Growth control rate of more than 90% (almost completely withered)

4: Growth control rate of from 70 to 90%

3: Growth control rate of from 40 to 70%

2: Growth control rate of from 20 to 40%

1: Growth control rate of from 5 to 20%

0: Growth control rate of less than 5% (almost non-effective)

The above growth control rates were calculated by the following equation: ##EQU1## where T: Weight of the weed grown above the soil surface of the treated area

N: Weight of the weed grown above the soil surface of the non-treated area

TEST EXAMPLE 2

Test on the herbicidal effects in foliage treatment

A plastic box having a length of 15 cm, a width of 22 cm and a depth of 6 cm was filled with a sterilized diluvial soil, and seeds of Echinochloa crus-galli, Digitaria adscendens, Cyperus microiria, Solanum nigrum, Galinsoga ciliata, Rorippa indica, oryza sativa, Zea mays, Triticum aestivum, Glycine max, Gossypium herbaceum and Beta vulgaris were spot-wisely sown. When the various weeds and crop plants grew to the 2 or 3 leaf stage, a herbicidal solution was uniformly sprayed on the foliages so that the active ingredient was applied in a predetermined concentration.

The herbicidal solution was prepared by diluting the formulation as described in the above Formulation Examples with water and applied onto the entire surface of the foliages of the weeds and the crop plants by a small spray. Three weeks after the application of the herbicide solution, the herbicidal effects against each weed and the phytotoxicities against each crop plant were determined on the basis of the standard ratings described in Test Example 1. The results are shown in Table 16.

In each Table, Compound Nos. correspond to Compound Nos. in the Examples, and symbols have the following meanings.

Dose: Dose of active ingredient (kg/ha)

N: Echinochloa crus-galli (barnyardgrass)

M: Digitaria adscendens (large crabgrass)

K: Cyperus microiria (annual sedge)

H: Solanum nigrum (black nightshade)

D: Galinsoga ciliata (hairy galinsoga)

I Rorippa indica (fieldcress)

R: Oryza sativa (rice)

T: Zea mays (corn)

S: Glycine max (soybean)

C: Gossypium herbaceum (cotton)

B: Beta vulgaris (sugar beet)

                  TABLE 15
    ______________________________________
    Comp. Dose
                                 No. (kg/ha) N M K H D I R T W S C
    ______________________________________
     1    0.16     1     2   2   4   5   5   0   0   0   3
                                 2
                                  0.32 2 3 3 5 5 5 0 0 0 4 3
                                  0.63 3 4 4 5 5 5 2 1 1 5 4
                                  2 0.16 2 3 3 5 5 5 3 0 0 2 3
                                  0.32 4 4 4 5 5 5 4 1 1 3 4
                                  0.63 5 5 5 5 5 5 5 2 4 4 5
                                  3 0.16 2 2 2 5 5 5 0 0 0 2 2
                                  0.32 3 4 4 5 5 5 1 0 1 3 3
                                  0.63 4 5 5 5 5 5 3 1 3 4 4
                                  4 0.16 1 1 1 4 5 5 1 0 0 1 1
                                  0.32 2 2 2 5 5 5 2 0 0 2 2
                                  0.63 3 3 3 5 5 5 4 1 1 3 4
                                  5 0.16 3 3 3 5 5 5 0 0 0 2 2
                                  0.32 4 3 4 5 5 5 1 1 1 3 3
                                  0.63 5 4 5 5 5 5 2 3 3 4 4
                                  6 0.16 2 2 1 5 5 5 3 0 0 2 3
                                  0.32 4 4 2 5 5 5 4 0 1 3 4
                                  0.63 5 5 3 5 5 5 5 2 4 4 5
                                  7 0.63 3 4 4 5 5 5 3 0 0 2 2
                                  8 0.16 1 2 2 4 5 5 3 0 0 2 2
                                  0.32 2 2 2 5 5 5 4 0 0 3 3
                                  0.63 3 3 3 5 5 5 5 1 2 3 4
                                  9 0.16 0 0 0 3 5 5 0 0 0 0 0
                                  0.32 1 1 1 4 5 5 0 0 0 1 1
                                  0.63 2 2 3 5 5 5 0 0 0 2 2
                                 10 0.16 0 1 0 3 5 5 0 0 0 1 0
                                  0.32 1 2 1 4 5 5 1 0 0 2 1
                                  0.63 2 3 2 5 5 5 2 0 0 3 3
                                 11 0.16 4 4 4 5 5 5 0 0 0 3 3
                                  0.32 5 5 4 5 5 5 1 0 0 4 3
                                  0.63 5 5 5 5 5 5 4 0 1 4 4
                                 14 0.04 1 2 1 5 5 5 2 0 0 0 0
                                  0.08 2 4 2 5 5 5 3 0 0 1 1
                                  0.16 3 5 4 5 5 5 3 1 2 4 2
                                 15 0.04 1 2 1 4 5 5 0 0 0 1 0
                                  0.08 2 3 2 5 5 5 0 0 0 2 1
                                  0.16 3 4 3 5 5 5 0 0 0 2 3
                                 16 0.63 1 3 3 4 5 5 1 0 0 1 0
                                 17 0.63 3 4 3 5 5 5 0 0 0 4 2
                                 19 0.16 0 1 1 5 4 5 0 0 0 0 0
                                  0.32 1 1 2 5 5 5 0 0 0 1 1
                                  0.63 2 3 3 5 5 5 0 0 0 2 2
                                 20 0.16 2 1 1 5 4 5 0 0 0 2 1
                                  0.32 3 1 2 5 5 5 0 0 0 3 2
                                  0.63 4 2 3 5 5 5 2 0 0 4 4
                                 21 0.16 3 3 4 5 5 5 2 0 1 2 2
                                  0.32 4 4 5 5 5 5 3 0 2 3 3
                                  0.63 5 5 5 5 5 5 4 1 3 4 4
                                 22 0.16 2 3 4 5 5 5 4 0 4 0 2
                                  0.32 4 4 5 5 5 5 5 1 5 1 3
                                  0.63 5 5 5 5 5 5 5 2 5 3 4
                                 23 0.63 1 2 3 5 5 5 0 0 0 0 2
                                 27 0.63 2 3 2 5 5 5 3 0 3 4 3
                                 28 0.63 2 3 3 5 5 5 2 0 4 4 4
                                 32 0.63 1 2 1 5 5 5 0 0 1 2 1
                                 33 0.16 1 1 0 5 5 4 0 0 0 3 0
                                  0.32 3 4 1 5 5 5 2 0 1 4 1
                                  0.63 5 5 3 5 5 5 4 1 3 5 2
                                 34 0.63 1 2 2 4 5 5 3 0 1 4 4
                                 35 0.63 1 2 1 4 5 5 0 1 0 3 3
                                 42 0.63 3 4 3 5 5 5 5 3 3 4 3
                                 43 0.16 2 3 3 4 5 5 3 0 0 1 2
                                  0.32 3 4 3 5 5 5 4 1 0 2 3
                                  0.63 4 4 4 5 5 5 4 2 0 4 4
                                 47 0.63 4 5 3 4 5 4 4 1 1 0 0
                                 48 0.16 0 1 2 4 4 5 0 0 0 1 1
                                  0.32 1 2 3 5 5 5 0 0 0 2 2
                                  0.63 2 4 4 5 5 5 1 0 0 3 2
                                 49 0.16 2 4 1 4 5 5 3 0 2 2 3
                                  0.32 3 5 2 5 5 5 4 0 3 3 3
                                  0.63 4 5 3 5 5 5 5 1 4 4 4
                                 52 0.16 2 3 2 5 5 5 4 0 2 4 4
                                  0.32 3 4 3 5 5 5 5 1 3 5 5
                                  0.63 3 4 3 5 5 5 5 2 3 5 5
                                 53 0.16 2 4 2 5 5 5 5 0 4 5 4
                                  0.32 4 5 3 5 5 5 5 1 5 5 5
                                  0.63 5 5 4 5 5 5 5 3 5 5 5
                                 55 0.16 1 1 2 4 5 5 2 0 0 0 0
                                  0.32 2 3 3 5 5 5 3 0 1 1 1
                                  0.63 4 5 4 5 5 5 4 0 3 4 3
    ______________________________________


TABLE 16 ______________________________________ Dose Comp. (kg/ No. ha) N M K H D I R T W S C B ______________________________________ 1 0.16 1 0 0 5 5 5 0 0 0 5 5 5 0.32 2 1 1 5 5 5 0 0 0 5 5 5 0.63 3 2 3 5 5 5 1 1 1 5 5 5 2 0.16 3 1 1 5 5 5 2 0 0 4 5 5 0.32 4 2 2 5 5 5 3 0 0 5 5 5 0.63 5 3 3 5 5 5 4 1 1 5 5 5 3 0.16 3 1 1 5 5 5 0 0 0 4 3 5 0.32 4 2 2 5 5 5 0 0 0 5 4 5 0.63 5 3 3 5 5 5 1 1 1 5 5 5 4 0.16 2 1 1 5 5 5 0 0 0 4 4 5 0.32 2 2 2 5 5 5 1 0 0 5 5 5 0.63 3 3 3 5 5 5 3 1 1 5 5 5 5 0.16 3 1 1 5 5 5 2 0 0 3 4 5 0.32 4 2 2 5 5 5 3 1 0 4 5 5 0.63 5 4 3 5 5 5 4 2 2 5 5 5 6 0.16 3 2 1 5 5 5 2 0 0 3 4 5 0.32 4 3 2 5 5 5 3 1 0 4 5 5 0.63 5 4 3 5 5 5 4 2 1 4 5 5 7 0.63 2 1 2 5 5 5 1 0 0 4 3 5 8 0.16 2 1 1 5 5 5 2 0 0 2 3 4 0.32 3 2 2 5 5 5 2 0 0 3 4 5 0.63 5 3 3 5 5 5 3 1 0 4 4 5 9 0.16 0 0 0 5 5 5 0 0 0 4 2 4 0.32 1 1 1 5 5 5 0 0 0 5 3 5 0.63 3 2 2 5 5 5 0 1 0 5 4 5 10 0.16 1 0 0 5 5 5 0 0 0 5 2 4 0.32 2 1 1 5 5 5 0 0 0 5 3 5 0.63 4 2 2 5 5 5 0 0 0 5 4 5 11 0.16 3 2 2 5 5 5 1 0 0 4 4 5 0.32 4 3 3 5 5 5 2 0 0 5 5 5 0.63 5 4 3 5 5 5 3 1 1 5 5 5 14 0.04 0 0 0 5 5 5 0 0 0 2 2 5 0.08 1 1 1 5 5 5 1 0 0 3 4 5 0.16 2 1 2 5 5 5 2 0 0 5 5 5 15 0.04 1 1 0 5 5 5 0 0 0 4 3 5 0.08 2 2 1 5 5 5 0 0 0 5 4 5 0.16 3 3 2 5 5 5 0 0 0 5 5 5 16 0.16 0 0 0 5 5 5 0 0 0 2 1 4 0.32 1 1 1 5 5 5 0 0 0 3 2 5 0.63 2 2 2 5 5 5 0 0 0 4 3 5 17 0.16 1 0 1 5 5 5 0 0 0 5 3 3 0.32 1 1 1 5 5 5 0 0 0 5 4 4 0.63 2 2 2 5 5 5 0 0 0 5 5 5 18 0.63 2 1 2 5 5 5 0 0 0 4 2 2 19 0.16 1 0 1 5 5 5 0 0 0 2 2 4 0.32 1 1 1 5 5 5 0 0 0 3 3 5 0.63 2 2 2 5 5 5 1 1 0 4 4 5 20 0.16 0 0 1 5 5 4 0 0 0 4 3 4 0.32 1 1 1 5 5 5 0 0 0 4 4 5 0.63 2 2 2 5 5 5 1 1 0 5 5 5 21 0.16 1 1 1 5 5 5 2 0 0 5 4 5 0.32 2 2 1 5 5 5 2 0 0 5 5 5 0.63 3 3 2 5 5 5 3 1 0 5 5 5 22 0.16 1 1 1 5 5 5 1 0 0 1 5 5 0.32 2 2 2 5 5 5 2 0 0 2 5 5 0.63 3 4 3 5 5 5 3 1 1 3 5 5 23 0.16 0 0 1 5 5 5 0 0 0 1 2 2 0.32 1 1 2 5 5 5 0 0 0 2 3 3 0.63 2 2 3 5 5 5 0 0 0 3 4 3 24 0.16 0 0 0 5 5 5 0 0 0 2 3 4 0.32 1 1 1 5 5 5 0 0 0 2 4 4 0.63 1 2 2 5 5 5 0 0 0 3 5 5 26 0.63 3 2 2 4 5 5 3 0 0 5 3 4 27 0.16 2 2 0 5 5 5 2 0 0 5 2 5 0.32 3 2 1 5 5 5 3 0 1 5 3 5 0.63 3 3 2 5 5 5 4 1 2 5 3 5 28 0.16 1 1 1 5 5 5 0 0 0 5 2 5 0.32 2 2 2 5 5 5 1 0 1 5 3 5 0.63 3 3 3 5 5 5 2 1 3 5 4 5 29 0.63 2 1 1 4 5 5 2 2 1 5 2 5 31 0.16 0 0 0 4 5 5 0 0 0 4 3 3 0.32 1 1 1 5 5 5 0 0 0 5 4 5 0.63 2 2 2 5 5 5 1 0 0 5 5 5 32 0.16 0 0 0 5 5 5 0 0 0 4 2 4 0.32 1 1 1 5 5 5 0 0 0 5 2 5 0.63 3 2 2 5 5 5 1 1 1 5 3 5 33 0.04 0 0 0 5 5 5 0 0 0 5 1 3 0.08 1 1 1 5 5 5 0 0 0 5 2 4 0.16 2 2 3 5 5 5 1 1 0 5 2 4 34 0.04 0 0 0 4 5 5 0 0 0 4 2 2 0.08 0 0 0 5 5 5 0 0 0 5 3 3 0.16 1 1 1 5 5 5 0 0 1 5 4 5 35 0.16 1 1 0 5 5 5 0 0 0 5 2 4 0.32 2 2 1 5 5 5 0 1 0 5 3 5 0.63 3 3 2 5 5 5 2 2 1 5 4 5 36 0.16 0 0 0 3 4 5 0 0 0 4 0 1 0.32 1 1 0 5 5 5 0 0 0 4 0 2 0.63 2 2 1 5 5 5 0 0 0 5 1 3 37 0.04 0 0 0 4 5 5 0 0 0 4 1 3 0.08 0 0 0 5 5 5 0 0 0 5 2 3 0.16 1 1 1 5 5 5 0 0 0 5 2 4 38 0.63 3 2 1 5 5 5 1 1 2 4 3 4 42 0.16 0 0 0 5 5 5 1 0 0 4 3 4 0.32 1 1 1 5 5 5 2 1 0 5 4 5 0.63 2 3 2 5 5 5 3 3 0 5 5 5 43 0.04 0 0 0 5 5 5 0 0 0 4 3 4 0.08 0 0 0 5 5 5 1 0 0 5 4 5 0.16 1 1 1 5 5 5 2 0 0 5 4 5 47 0.04 0 0 0 5 5 5 0 0 0 4 3 1 0.08 1 1 1 5 5 5 0 0 0 5 4 2 0.16 2 2 2 5 5 5 1 0 0 5 4 4 48 0.16 0 0 1 5 5 5 0 0 0 3 4 5 0.32 1 1 2 5 5 5 0 0 0 4 5 5 0.63 2 3 3 5 5 5 1 0 0 5 5 5 49 0.16 2 1 0 5 5 5 0 0 0 5 5 5 0.32 3 2 1 5 5 5 0 0 0 5 5 5 0.63 4 3 2 5 5 5 1 1 1 5 5 5 50 0.63 2 2 1 5 5 5 1 0 0 2 3 4 52 0.16 3 1 1 5 5 5 3 1 0 5 5 5 0.32 4 2 2 5 5 5 4 2 1 5 5 5 0.63 5 3 3 5 5 5 4 3 2 5 5 5 53 0.16 4 3 2 5 5 5 2 1 0 5 5 5 0.32 5 4 3 5 5 5 3 2 1 5 5 5 0.63 5 5 4 5 5 5 4 4 3 5 5 5 55 0.16 2 1 1 4 5 5 0 0 0 3 2 3 0.32 3 2 2 5 5 5 1 0 0 4 3 4 0.63 4 3 4 5 5 5 2 0 1 5 4 4 ______________________________________



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